Sunitinib malate
别名: SU11248 malate 中文名称：苹果酸舒尼替尼
Sunitinib malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，在无细胞试验中IC50分别为80 nM 和2 nM，也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。
Sunitinib malate Chemical Structure
CAS: 341031-54-7
产品质控
批次：
纯度：
99.60%
99.60
Sunitinib malate相关产品
| 相关靶点 | PDGFRα PDGFRβ | 点击展开 |
|---|---|---|
| 相关产品 | Crenolanib CP-673451 Orantinib (SU6668) Tyrphostin AG 1296 Trapidil PP121 AZD2932 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| U251 | Kinase Assay | 10 μM | 1 h | Inhibition of VEGFR2 with IC50 of 0.0189 μM | 24890652 |
| SH-SY5Y | Kinase Assay | 10 μM | 1 h | Inhibition of PDGFRbeta with IC50 of 0.0831 μM | 24890652 |
| A431 | Kinase Assay | 10 μM | 1 h | Inhibition of EGFR with IC50 of 0.1721 μM | 24890652 |
| HUVEC | Growth Inhibition Assay | 3 μM | 24 h | Antiangiogenic activity assessed as inhibition of VEGF-induced tube formation with EC50 of 0.645 μM | 23583911 |
| A498 | Cytotoxic Assay | 100 μM | 72 h | IC50=4.3 μM | 23489626 |
| HUVEC | Function Assay | 2 μM | 18 h | Antiangiogenic activity in HUVECs under hypoxic condition assessed as inhibition of tube formation | 23153200 |
| HT-29 | Cytotoxic Assay | 100 μM | 72 h | Cytotoxicity against VEGFR expressing human HT-29 cells with IC50 of 0.33 μM | 23131541 |
| HAEC | Cytotoxic Assay | 100 μM | 72 h | Cytotoxicity against VEGFR expressing HAEC with IC50 of 0.1 μM | 23131541 |
| UACC257 | Growth Inhibition Assay | 100 μM | 48 h | GI57=4 μM | 22560627 |
| TK10 | Growth Inhibition Assay | 100 μM | 48 h | GI56=6.3 μM | 22560627 |
| SW620 | Growth Inhibition Assay | 100 μM | 48 h | GI55=1.3 μM | 22560627 |
| SNB19 | Growth Inhibition Assay | 100 μM | 48 h | GI54=10 μM | 22560627 |
| OVCAR3 | Growth Inhibition Assay | 100 μM | 48 h | GI53=3.2 μM | 22560627 |
| MDA-MB-435 | Growth Inhibition Assay | 100 μM | 48 h | GI52=2 μM | 22560627 |
| MCF7 | Growth Inhibition Assay | 100 μM | 48 h | GI51=2 μM | 22560627 |
| EKVX | Growth Inhibition Assay | 100 μM | 48 h | GI50=7.9 μM | 22560627 |
| CAKI-1 | Growth Inhibition Assay | 100 μM | 48 h | GI50=0.63 μM | 22560627 |
| HT-29 | Growth Inhibition Assay | 100 μM | 72 h | Antiproliferative activity against human HT-29 cells expressing VEGFR with IC50 of 0.33 μM | 22444679 |
| HAEC | Growth Inhibition Assay | 100 μM | 72 h | Antiproliferative activity against human HAEC cells expressing VEGFR with IC50 of 0.1 μM | 22444679 |
| SF-539 | Kinase Assay | 333 μM | 60 min | Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells with IC50 of 12.2 μM | 22204741 |
| PC3 | Cytotoxic Assay | 50 μM | 48 h | IC50=25.1 μM | 22019188 |
| K562 | Cytotoxic Assay | 50 μM | 48 h | IC50=21.9 μM | 22019188 |
| HL60 | Cytotoxic Assay | 50 μM | 48 h | IC50=15.5 μM | 22019188 |
| HUVEC | Function Assay | 1 μM | 1 h | does not inhibit AKT phosphorylation at Ser-473 in VEGF-stimulated HUVEC | 21963305 |
| HUVEC | Kinase Assay | 1 μM | 1 h | Inhibition of VEGFR2 phosphorylation at tyr-1175 in VEGF-stimulated HUVEC | 21963305 |
| HUVEC | Function Assay | 1 μM | 1 h | Inhibition of eNOS phosphorylation at Ser-1172 in VEGF-stimulated HUVEC | 21963305 |
| HUVEC | Function Assay | 1 μM | 1 h | Inhibition of ERK phosphorylation at Thr202/Tyr204 in VEGF-stimulated HUVEC | 21963305 |
| HUVEC | Function Assay | 1 μM | 24 h | Antiangiogenic activity assessed as decrease in VEGF-induced cell migration | 21963305 |
| HEK293 | Kinase Assay | 100 nM | 1 h | does not inhibit VEGF-induced autophosphorylation of tyrosine 1175 residue on VEGFR2 expressed in HEK293 cells | 21885287 |
| U251 | Kinase Assay | 333 μM | 60 min | Inhibition of VEGFR2 phosphorylation with IC50 of 18.9 μM | 20403700 |
| SF-539 | Kinase Assay | 333 μM | 60 min | Inhibition of PDGFRbeta phosphorylation with IC50 of 12.2 μM | 20403700 |
| HUVEC | Antiangiogenic assay | 10 uM | 5 hrs | Antiangiogenic activity in human HUVEC cells assessed as angiogenesis rate at 10 uM after 5 hrs by endothelial tube formation assay relative to control | 26912111 |
| MCF7 | Function assay | 1 uM | 24 hrs | Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated ERK1/2 at 1 uM incubated for 24 hrs by Western blot analysis | 27176944 |
| MCF7 | Function assay | 1 uM | 24 hrs | Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated Raf1 at 1 uM incubated for 24 hrs by Western blot analysis | 27176944 |
| MCF7 | Function assay | 4 uM | 24 hrs | Inhibition of VEGFR2 phosphorylation in human MCF7 cells at 4 uM incubated for 24 hrs by Western blot method | 28942113 |
| HUVEC | Kinase Assay | 200 μM | Inhibition of VEGFR1 phosphorylation in growth factor-stimulated HUVEC | 23583911 | |
| HUVEC | Kinase Assay | 200 μM | Inhibition of VEGFR2 phosphorylation in growth factor-stimulated HUVEC | 23583911 | |
| H4 | Cytotoxic Assay | 10 μM | Toxicity in human H4 cells | 20350806 | |
| ACHN | Cytotoxicity assay | 72 hrs | Cytotoxicity against human ACHN cells after 72 hrs by MTT assay, IC50 = 2 μM. | 25124114 | |
| THP1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0457 μM. | 25089810 | |
| HL60 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0368 μM. | 25089810 | |
| MV4-11 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0243 μM. | 25089810 | |
| MOLM13 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0177 μM. | 25089810 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 13.6 μM. | 25064347 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 10.5 μM. | 25064347 | |
| U251 | Function assay | 60 mins | Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA, IC50 = 18.9 μM. | 23434139 | |
| U251 | Function assay | 60 mins | Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 18.9 μM. | 23375090 | |
| U251 | Function assay | 60 mins | Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 18.9 μM. | 22739090 | |
| primary leukemia cells | Cytotoxicity assay | 72 hrs | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 1.1 μM. | 22221201 | |
| primary leukemia cells | Cytotoxicity assay | 72 hrs | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM. | 22221201 | |
| primary leukemia cells | Cytotoxicity assay | 72 hrs | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM. | 22221201 | |
| FDC-P1 | Function assay | 48 hrs | Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay, IC50 = 0.155 μM. | 20156689 | |
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay, IC50 = 0.0043 μM. | 19754199 | |
| 3T3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse 3T3 cells expressing human CSF1R after 72 hrs by Celltiter assay, Activity = 0.09 μM. | 18694641 | |
| TT | Growth Inhibition Assay | 72 h | IC50=0.04 μM | 24904961 | |
| NCI-H526 | Growth Inhibition Assay | 72 h | IC50=1.01 μM | 24904961 | |
| NCI-H460 | Growth Inhibition Assay | 72 h | IC50=4.31 μM | 24904961 | |
| NCI-H3122 | Growth Inhibition Assay | 72 h | IC50=0.83 μM | 24904961 | |
| MV4-11 | Growth Inhibition Assay | 48 h | IC50=0.003 μM | 24904961 | |
| LO2 | Growth Inhibition Assay | 72 h | IC50=19.93 μM | 24904961 | |
| HK2 | Growth Inhibition Assay | 72 h | IC50=5.85 μM | 24904961 | |
| Bel7402 | Growth Inhibition Assay | 72 h | IC50=2.67 μM | 24904961 | |
| MDA-MB-468 | Cytotoxic Assay | 72 h | IC50=0.0061 μM | 24890652 | |
| MDA-MB-435 | Cytotoxic Assay | 72 h | IC50=0.0097 μM | 24890652 | |
| MDA-MB-231 | Cytotoxic Assay | 72 h | IC50=0.0223 μM | 24890652 | |
| MCF7 | Cytotoxic Assay | 72 h | IC50=0.0293 μM | 24890652 | |
| MCF7 | Cytotoxic Assay | 72 h | IC50=0.0271 μM | 24890652 | |
| 4T1 | Cytotoxic Assay | 72 h | IC50=0.016 μM | 24890652 | |
| T24 | Growth Inhibition Assay | 72 h | IC50=2.44 μM | 23999040 | |
| HT-29 | Growth Inhibition Assay | 72 h | IC50=1.47 μM | 23999040 | |
| BxPC3 | Growth Inhibition Assay | 72 h | IC50=3.63 μM | 23999040 | |
| BGC | Growth Inhibition Assay | 72 h | IC50=4.78 μM | 23999040 | |
| MCF7 | Cytotoxic Assay | 72 h | IC50=6.29 μM | 23602441 | |
| HCT116 | Cytotoxic Assay | 72 h | IC50=4.71 μM | 23602441 | |
| A549 | Cytotoxic Assay | 72 h | IC50=2.44 μM | 23602441 | |
| ACHN | Cytotoxic Assay | 6 d | IC50=2.5 μM | 23360104 | |
| HCT116 | Function Assay | 24 h | Antimigratory activity assessed as inhibition of cell migration | 23153200 | |
| PC9 | Cytotoxic Assay | 48 h | IC50=10.97 μM | 22483608 | |
| HepG2 | Cytotoxic Assay | 48 h | IC50=13.24 μM | 22483608 | |
| MV4-11 | Cytotoxic Assay | 72 h | IC50=0.003 μM | 22452518 | |
| WI38 | Cytotoxic Assay | 72 h | IC50=8.56 μM | 21621880 | |
| SMMC7721 | Cytotoxic Assay | 72 h | IC50=6.47 μM | 21621880 | |
| H460 | Cytotoxic Assay | 72 h | IC50=2.7 μM | 21621880 | |
| MDA-MB-231 | Growth Inhibition Assay | 16 h | Antitumor activity against human MDA-MB-231 cells | 21450463 | |
| K562 | Growth Inhibition Assay | 16 h | Antitumor activity against human K562 cells | 21450463 | |
| IM9 | Growth Inhibition Assay | 16 h | Antitumor activity against human IM9 cells | 21450463 | |
| HUVEC | Growth Inhibition Assay | 16 h | Inhibition of bFGF-induced cell proliferation with IC50 of 4.04 μM | 21450463 | |
| HUVEC | Growth Inhibition Assay | 16 h | Inhibition of VEGF-induced cell proliferation with IC50 of 2.75 μM | 21450463 | |
| HL60 | Growth Inhibition Assay | 16 h | Antitumor activity against human HL60 cells | 21450463 | |
| A549 | Growth Inhibition Assay | 16 h | Antitumor activity against human A549 cells | 21450463 | |
| THP1 | Growth Inhibition Assay | 72 h | IC50=0.5 μM | 20570526 | |
| RS4-11 | Growth Inhibition Assay | 72 h | IC50=1 μM | 20570526 | |
| Kasumi-1 | Growth Inhibition Assay | 72 h | IC50=0.016 μM | 20570526 | |
| HepG2 | Growth Inhibition Assay | 72 h | IC50=3.81 μM | 20570526 | |
| Sf9 | Function Assay | 1 h | Inhibition of human recombinant His-tagged RET expressed with IC50 of 1.3 μM | 20117004 | |
| BaPTC2 | Growth Inhibition Assay | 72 h | IC50=0.22 μM | 20117004 | |
| Ba/F3 | Growth Inhibition Assay | 72 h | IC50=1.2 μM | 20117004 | |
| Sf9 | Kinase Assay | 30 min | Inhibition of GST-tagged VEGFR expressed with IC50 of 0.185 μM | 19854051 | |
| RS4-11 | Function Assay | 2 h | Inhibition of FLT3 ITD mutant autophosphorylation with IC50 of 0.034 μM | 19654408 | |
| RS4-11 | Function Assay | 2 h | Inhibition of FLT3 autophosphorylation with IC50 of 0.0099 μM | 19654408 | |
| A375 | Cytotoxic Assay | 72 h | IC50=5.4 μM | 19654408 | |
| KBV1 | Cytotoxic Assay | 72 h | Cytotoxicity against human P-glycoprotein-expressing KBV1 cells with IC50 of 4.1 μM | 19397322 | |
| KB3-1 | Cytotoxic Assay | 72 h | Cytotoxicity against human P-gp-negative KB-3-1 cells with IC50 of 2.3 μM | 19397322 | |
| NIH3T3 | Kinase Assay | 20 min | inhibit human KDR kinase expressed with IC50 of 0.018 μM | 16162008 | |
| 3T3 | Kinase Assay | 20 min | Cellular inhibition of VEGF induced human KDR phosphorylation with IC50 of 0.022 μM | 16162008 | |
| U251 | Function assay | 60 min | Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0189 μM. | 25882519 | |
| U251 | Function assay | 60 min | Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0831 μM. | 25882519 | |
| A431 | Function assay | 60 min | Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.1721 μM. | 25882519 | |
| HT-29 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HT-29 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 4.7 μM. | 26009164 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 7.93 μM. | 26009164 | |
| SKOV3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SKOV3 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 9.21 μM. | 26009164 | |
| PANC1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PANC1 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 14.94 μM. | 26009164 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 16.06 μM. | 26009164 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 25.41 μM. | 26009164 | |
| Bel7402 | Photocytotoxicity assay | 5 hrs | Photocytotoxicity against human Bel7402 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 11 μM. | 26584085 | |
| PANC1 | Photocytotoxicity assay | 5 hrs | Photocytotoxicity against human PANC1 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 13 μM. | 26584085 | |
| SVEC4-10 | Cytotoxicity assay | 24 hrs | Cytotoxicity against mouse SVEC4-10 cells assessed as cell viability after 24 hrs by MTS assay, IC50 = 8 μM. | 26912111 | |
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against FLT3-ITD dependent human MV4-11 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM. | 27077705 | |
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.002 μM. | 27077705 | |
| MOLM14 | Antiproliferative assay | 72 hrs | Antiproliferative activity against FLT3-ITD dependent human MOLM14 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.005 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.006 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.009 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.02 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.023 μM. | 27077705 | |
| GISTT1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.041 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.053 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.078 μM. | 27077705 | |
| GIST882 | Antiproliferative assay | 72 hrs | Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.11 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.51 μM. | 27077705 | |
| Rec1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Rec1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.87 μM. | 27077705 | |
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1 μM. | 27077705 | |
| KU812 | Antiproliferative assay | 72 hrs | Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.1 μM. | 27077705 | |
| BCR-ABL dependent MEG01 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.2 μM. | 27077705 | |
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.38 μM. | 27077705 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.7 μM. | 27077705 | |
| GIST48B | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GIST48B cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.01 μM. | 27077705 | |
| CHO | Antiproliferative assay | 72 hrs | Antiproliferative activity against CHO cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.03 μM. | 27077705 | |
| CHL | Antiproliferative assay | 72 hrs | Antiproliferative activity against CHL cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.48 μM. | 27077705 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 7.4 μM. | 27128173 | |
| BT549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT549 cells after 48 hrs by MTT assay, IC50 = 15.5 μM. | 27128173 | |
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells after 48 hrs by MTT assay, IC50 = 16.4 μM. | 27128173 | |
| PC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 19.6 μM. | 27128173 | |
| RWPE1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RWPE1 cells after 48 hrs by MTT assay, IC50 = 23 μM. | 27128173 | |
| PA1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 7.97 μM. | 27210438 | |
| LNCAP | Cytotoxicity assay | 48 hrs | Cytotoxicity against human LNCAP cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 12.61 μM. | 27210438 | |
| RWPE1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RWPE1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23 μM. | 27210438 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23.76 μM. | 27210438 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 7.44 μM. | 27448916 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 14.4 μM. | 27448916 | |
| BT549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 15.54 μM. | 27448916 | |
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 16.38 μM. | 27448916 | |
| PC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 19.6 μM. | 27448916 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 23.8 μM. | 27448916 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 7.4 μM. | 27639369 | |
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 10.4 μM. | 27639369 | |
| PC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 12.6 μM. | 27639369 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 14.4 μM. | 27639369 | |
| BT549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 15.5 μM. | 27639369 | |
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 16.3 μM. | 27639369 | |
| RWPE1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RWPE1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 25.2 μM. | 27639369 | |
| L02 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human L02 cells after 72 hrs by CCK-8 assay, IC50 = 4.62 μM. | 27643639 | |
| HL60 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HL60 cells after 72 hrs by CCK-8 assay, IC50 = 4.95 μM. | 27643639 | |
| U251 | Function assay | 60 mins | Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method, IC50 = 0.0189 μM. | 27894589 | |
| SF539 | Function assay | 60 mins | Inhibition of PDGFR-beta in human SF539 cells assessed as reduction in PDGF-BB induced phosphorylation preincubated for 60 mins followed by PDGF-BB addition measured after 10 mins by ELISA method, IC50 = 0.0831 μM. | 27894589 | |
| HuH7 | Growth inhibition assay | 48 hrs | Growth inhibition of human HuH7 cells after 48 hrs by MTT assay, IC50 = 3.03 μM. | 27956344 | |
| HCT116 | Growth inhibition assay | 48 hrs | Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50 = 5.62 μM. | 27956344 | |
| SW620 | Growth inhibition assay | 48 hrs | Growth inhibition of human SW620 cells after 48 hrs by MTT assay, IC50 = 6.25 μM. | 27956344 | |
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant after 72 hrs by MTS assay, IC50 = 0.0385 μM. | 28038328 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 16.06 μM. | 28057423 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 25.41 μM. | 28057423 | |
| HEK293 | Function assay | 2 mins | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay, IC50 = 6.1 μM. | 28230985 | |
| RCC4 | Anticancer assay | 48 hrs | Anticancer activity against human RCC4 cells after 48 hrs by XTT assay, IC50 = 4 μM. | 28325600 | |
| MDA-MB-231 | Anticancer assay | 48 hrs | Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay, IC50 = 6 μM. | 28325600 | |
| COLO205 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay, IC50 = 8 μM. | 28756024 | |
| K562 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50 = 14 μM. | 28756024 | |
| MDA-MB-231 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 32 μM. | 28756024 | |
| MDA-MB-231 | Cytotoxicity assay | 24 hrs | Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay, IC50 = 6.98 μM. | 28760313 | |
| GISTT1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.04 μM. | 28991465 | |
| GISTT1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.09 μM. | 28991465 | |
| GIST430 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.098 μM. | 28991465 | |
| GISTT1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 5.88 μM. | 28991465 | |
| HuH7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.707 μM. | 29057042 | |
| A498 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 7.981 μM. | 29057042 | |
| NCI-H727 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 10.12 μM. | 29057042 | |
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50 = 0.01 μM. | 29935772 | |
| U251 | Function assay | 60 mins | Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA, IC50 = 0.0189 μM. | 30098869 | |
| SH-SY5Y | Function assay | 60 mins | Inhibition of PDGF-BB-induced PDGFRbeta activation in human SH-SY5Y cells pretreated for 60 mins followed by PDGF-BB addition and measured after 10 mins by ELISA, IC50 = 0.0831 μM. | 30098869 | |
| A431 | Function assay | 60 mins | Inhibition of EGF-induced EGFR activation in human A431 cells pretreated for 60 mins followed by EGF addition and measured after 10 mins by ELISA, IC50 = 0.1721 μM. | 30098869 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.004 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.005 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.006 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.012 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.024 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.027 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.03 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.214 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.271 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.398 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.43 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.584 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.631 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.638 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.696 μM. | 30204441 | |
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.782 μM. | 30204441 | |
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 4.789 μM. | 30204441 | |
| Sf21 | Function assay | 60 mins | Inhibition of recombinant human N-terminal His6-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells after 60 mins by ELISA, IC50 = 0.0047 μM. | 30241010 | |
| HEK293 | Function assay | Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 39.8107 μM. | 25087753 | ||
| CHO K1 | Function assay | Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 15.8489 μM. | 25087753 | ||
| CHO K1 | Function assay | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform, IC50 = 10 μM. | 25087753 | ||
| CHO | Function assay | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform, IC50 = 7.94328 μM. | 25087753 | ||
| U251 | Function assay | Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50 = 0.0189 μM. | 24900865 | ||
| CHO | Function assay | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 33.4 μM. | 23812503 | ||
| endothelial precursor cells | Function assay | Inhibition of cell migration in endothelial precursor cells by Oris cell migration kit based phenotypic drug discovery based assay, IC50 = 13.6 μM. | 22409666 | ||
| endothelial precursor cells | Function assay | Inhibition of endothelial cord area formation in endothelial precursor cells by CD31 cord area detection based phenotypic drug discovery based assay, IC50 = 0.0096 μM. | 22409666 | ||
| HEK293 | Function assay | Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay, Kd = 0.00047 μM. | 19754199 | ||
| Kasumi-1 | Function Assay | Inhibition of c-Kit autophosphorylation with IC50 of 0.015 μM | 20833039 | ||
| A431 | Kinase Assay | Inhibition of VEGFR2 expressed with IC50 of 18.9 μM | 20558072 | ||
| A431 | Kinase Assay | Inhibition of PDGFRbeta expressed with IC50 of 12.2 μM | 20558072 | ||
| DU145 | Function Assay | Inhibition of c-Met dependent HGF-induced human DU145 cell scattering with IC50 of 10 μM | 18434145 | ||
| A549 | Function Assay | Inhibition of c-Met dependent HGF-induced human A549 cell migration with IC50 of 2 μM | 18434145 | ||
| 3T3 | Function Assay | Inhibition of Vascular endothelial growth factor receptor with IC50 of 0.05 μM | 12646019 | ||
| 3T3 | Growth Inhibition Assay | Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation with IC50 of 0.01 μM | 12646019 | ||
| 3T3 | Kinase Assay | Inhibition of PDGF-induced BrdU incorporation with IC50 of 0.007 μM | 12646019 | ||
| HT-29 | Cytotoxicity assay | Cytotoxicity against human HT-29 cells by MTT assay, IC50 = 1.7 μM. | 26920800 | ||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells by MTT assay, IC50 = 9.1 μM. | 26920800 | ||
| MDA-MB-435 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-435 cells by MTT assay, IC50 = 9.3 μM. | 26920800 | ||
| BAF3 | Antiproliferative assay | Antiproliferative activity against mouse BAF3 cells, GI50 = 2.78 μM. | 27077705 | ||
| CHO | Function assay | Inhibition of human ERG expressed in CHO cells by Qpatch assay, IC50 = 0.5 μM. | 28038328 | ||
| HuH7 | Antiproliferative assay | Antiproliferative activity against human HuH7 cells by MTT assay, IC50 = 3.03 μM. | 30059803 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 5.62 μM. | 30059803 | ||
| SW620 | Antiproliferative assay | Antiproliferative activity against human SW620 cells by MTT assay, IC50 = 6.25 μM. | 30059803 | ||
| HepG2 | Antiproliferative assay | Antiproliferative activity against human HepG2 cells by MTT assay, IC50 = 7.78 μM. | 30059803 | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=1.64 pM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=272 pM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=15.3 nM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=30.94 nM | SANGER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=33.8 nM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=79.89 nM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=98.52 nM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=350.14 nM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=507.61 nM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=614.25 nM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=631.32 nM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=710.23 nM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=804.55 nM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=981.06 nM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=1.11407 μM | SANGER | ||
| BL-70 | Growth Inhibition Assay | IC50=1.11846 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=1.2858 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=1.34141 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=1.36851 μM | SANGER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=1.37009 μM | SANGER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=1.46486 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=1.50676 μM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=1.54572 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=1.62546 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=1.69247 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=1.72751 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=1.81624 μM | SANGER | ||
| EMG-01 | Growth Inhibition Assay | IC50=1.83563 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=1.83985 μM | SANGER | ||
| CMK | Growth Inhibition Assay | IC50=1.95517 μM | SANGER | ||
| NB1 | Growth Inhibition Assay | IC50=1.96117 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=2.05946 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=2.08482 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=2.11137 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=2.11313 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=2.13508 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=2.17924 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=2.22375 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=2.33431 μM | SANGER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=2.33618 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=2.3366 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=2.34384 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=2.37038 μM | SANGER | ||
| K052 | Growth Inhibition Assay | IC50=2.40202 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.49446 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=2.60237 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=2.60339 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=2.63512 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=2.69545 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=2.72989 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=2.78304 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=2.79758 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=2.80628 μM | SANGER | ||
| SCC-3 | Growth Inhibition Assay | IC50=2.82891 μM | SANGER | ||
| NALM-6 | Growth Inhibition Assay | IC50=2.90473 μM | SANGER | ||
| BL-41 | Growth Inhibition Assay | IC50=2.91222 μM | SANGER | ||
| OPM-2 | Growth Inhibition Assay | IC50=3.05954 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=3.06198 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=3.23111 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=3.32869 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=3.39838 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=3.4457 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=3.48005 μM | SANGER | ||
| RPMI-6666 | Growth Inhibition Assay | IC50=3.54171 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=3.63391 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=3.67114 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=3.70508 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=3.78642 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=3.83338 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=3.83778 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=3.98832 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=4.06158 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=4.12168 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=4.20914 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=4.21065 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=4.3352 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=4.33699 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=4.36729 μM | SANGER | ||
| LC4-1 | Growth Inhibition Assay | IC50=4.3807 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=4.43081 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=4.55307 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=4.67099 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=4.67911 μM | SANGER | ||
| SU-DHL-1 | Growth Inhibition Assay | IC50=4.80174 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=4.80621 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=4.8731 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=5.17301 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=5.32312 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=5.43291 μM | SANGER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=5.4782 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=5.4837 μM | SANGER | ||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=5.76719 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=6.02878 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=6.07909 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=6.10949 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=6.12519 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=6.27517 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=6.32109 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=6.3471 μM | SANGER | ||
| DG-75 | Growth Inhibition Assay | IC50=6.43069 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=6.43207 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=6.51507 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=6.60763 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=6.6942 μM | SANGER | ||
| CESS | Growth Inhibition Assay | IC50=7.10438 μM | SANGER | ||
| BC-1 | Growth Inhibition Assay | IC50=7.24812 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=7.30389 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=7.3785 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=7.45804 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=7.50739 μM | SANGER | ||
| ARH-77 | Growth Inhibition Assay | IC50=7.53597 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=7.54088 μM | SANGER | ||
| IMR-5 | Growth Inhibition Assay | IC50=7054876 μM | SANGER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=7.57206 μM | SANGER | ||
| CA46 | Growth Inhibition Assay | IC50=7.58012 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=7.66061 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=7.77557 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=8.02417 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=8.11652 μM | SANGER | ||
| TALL-1 | Growth Inhibition Assay | IC50=8.18384 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=8.1942 μM | SANGER | ||
| HCC1599 | Growth Inhibition Assay | IC50=8.19987 μM | SANGER | ||
| CI-1 | Growth Inhibition Assay | IC50=8.20411 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=8.20661 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=8.23546 μM | SANGER | ||
| CPC-N | Growth Inhibition Assay | IC50=8.29199 μM | SANGER | ||
| MC-CAR | Growth Inhibition Assay | IC50=8.3358 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=8.34758 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=8.50351 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=8.56508 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=8.60985 μM | SANGER | ||
| NCCIT | Growth Inhibition Assay | IC50=8.71745 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=9.13834 μM | SANGER | ||
| COR-L279 | Growth Inhibition Assay | IC50=9.3909 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=9.68161 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=9.78083 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=9.79994 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=9.81016 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=9.99933 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=10.2207 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=10.2984 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=10.9277 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=11.265 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=11.4834 μM | SANGER | ||
| NCI-H2107 | Growth Inhibition Assay | IC50=11.5984 μM | SANGER | ||
| K562 | Growth Inhibition Assay | IC50=11.8702 μM | SANGER | ||
| LOUCY | Growth Inhibition Assay | IC50=11.9875 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=12.002 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=12.1565 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=12.2985 μM | SANGER | ||
| BC-3 | Growth Inhibition Assay | IC50=12.4651 μM | SANGER | ||
| REH | Growth Inhibition Assay | IC50=12.6498 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=12.6887 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=12.8694 μM | SANGER | ||
| NCI-H128 | Growth Inhibition Assay | IC50=13.0723 μM | SANGER | ||
| NCI-H1694 | Growth Inhibition Assay | IC50=13.1144 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=13.3276 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=13.345 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=13.6729 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=13.7294 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=13.7573 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=14.2457 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=14.2894 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=14.4169 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=14.5369 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=15.2251 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=16.0012 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=16.256 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=16.5931 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=16.8489 μM | SANGER | ||
| NCI-H719 | Growth Inhibition Assay | IC50=16.9161 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=16.9907 μM | SANGER | ||
| EVSA-T | Growth Inhibition Assay | IC50=17.0485 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=17.6913 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=17.8572 μM | SANGER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=17.9834 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=17.9904 μM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=18.0151 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=18.0187 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=18.0866 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=18.4162 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=18.5672 μM | SANGER | ||
| Raji | Growth Inhibition Assay | IC50=19.9565 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=20.4104 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=20.4293 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=20.5521 μM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=21.0264 μM | SANGER | ||
| GDM-1 | Growth Inhibition Assay | IC50=21.9414 μM | SANGER | ||
| KMS-12-PE | Growth Inhibition Assay | IC50=22.274 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=24.1278 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=24.7349 μM | SANGER | ||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=26.2742 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=27.1822 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=27.4946 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=27.9229 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=28.0074 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=28.2898 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=28.69 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=28.9195 μM | SANGER | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=29.0176 μM | SANGER | ||
| EB-3 | Growth Inhibition Assay | IC50=29.5309 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=29.619 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=30.126 μM | SANGER | ||
| COLO-668 | Growth Inhibition Assay | IC50=30.792 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=31.1063 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=31.6085 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=31.8678 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=32.3843 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=32.8485 μM | SANGER | ||
| EHEB | Growth Inhibition Assay | IC50=34.1193 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=34.2781 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=34.4725 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=37.0401 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=37.5004 μM | SANGER | ||
| NCI-H2141 | Growth Inhibition Assay | IC50=38.0843 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=42.0586 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=42.6405 μM | SANGER | ||
| LC-1F | Growth Inhibition Assay | IC50=43.3682 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=43.9359 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=44.1252 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=44.9577 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=49.8825 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Sunitinib malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，在无细胞试验中IC50分别为80 nM 和2 nM，也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Sunitinib也是有效的c-Kit抑制剂，IC50为211 nM。[1] Sunitinib是有效的ATP竞争性VEGFR2 (Flk1)和PDGFRβ抑制剂， Ki 分别为9 nM和 8 nM,作用于VEGFR2和 PDGFR 比作用于FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl,和 src选择性高10多倍。Sunitinib 作用于血清饥饿处理的表达VEGFR2或PDGFRβ的NIH-3T3细胞, 抑制VEGF依赖的 VEGFR2磷酸化和 PDGF依赖的PDGFRβ磷酸化，IC50分别为10 nM和 10 nM。Sunitinib抑制VEGF诱导的血清饥饿处理的 HUVECs 增殖，IC50为40 nM, 且抑制PDGF诱导的过量表达PDGFRβ或 PDGFRα的NIH-3T3细胞，IC50分别为39 nM和 69 nM。[2] Sunitinib 抑制野生型FLT3, FLT3-ITD,和FLT3-Asp835磷酸化，IC50分别为250 nM, 50 nM, 和 30 nM。Sunitinib 抑制MV4;11和 OC1-AML5细胞增殖，IC50分别为8 nM 和4 nM, 且诱导凋亡，这种作用存在剂量依赖性。 [3] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | RS4;11, MV4;11, 和 OC1-AML5 | ||
| 浓度 | 溶于DMSO,终浓度为~10 μM | |||
| 孵育时间 | 24 和48 小时 | |||
| 方法 | 细胞在含0.1% FBS 的培养基上饥饿处理过夜，然后加入Sunitinib和 FL (50 ng/mL; FLT3-WT)。培养48小时后，使用 Alamar Blue 检测或台酚蓝细胞活力检测测定增殖。加入Sunitinib 24小时后，测量凋亡，通过Western blotting测定caspase-3水平的PARP分裂。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK p-GSK3β / GSK3β / MYCN p-AKT / AKT / p-ERK / ERK |
|
19244102 | |
| Growth inhibition assay | Cell viability |
|
24369536 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 与体内大量且选择性抑制VEGFR2或PDGFR磷酸化和信号相一致, Sunitinib每天按 20-80 mg/kg 剂量处理多种移植瘤模型，包括HT-29, A431, Colo205, H-460, SF763T, C6, A375,或 MDA-MB-435，具有广泛且有效的抗癌活性，这种作用存在剂量依赖性。Sunitinib 每天按 80 mg/kg剂量处理，持续21天，使八只鼠中有六只肿瘤完全衰退，且在处理结束后，观察110天，肿瘤不会复发。使用 Sunitinib进行第二轮处理，仍然高效作用于第一轮没有完全衰退的肿瘤。Sunitinib处理SF763T胶质瘤，导致肿瘤MVD显著降低，降低~40%。SU11248 处理，完全抑制表达荧光素酶的PC-3M移植瘤生长，而肿瘤尺寸没有减小。[2] Sunitinib 每天按20 mg/kg剂量处理，显著阻断皮下MV4;11 (FLT3-ITD)移植瘤生长，且作用于FLT3-ITD骨髓移植瘤模型，抑制延长的寿命。[3] |
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|---|---|---|
| 动物实验 | Animal Models | 皮下移植 HT-29, A431, Colo205, H-460, SF763T, C6, A375,或 MDA-MB-435的雌性nu/nu小鼠,携带表达荧光素酶 PC-3M肿瘤的雄性nu/nu小鼠 |
| Dosages | ~80 mg/kg | |
| Administration | 口服处理，每天一次 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06222593 | Not yet recruiting | Carcinoma Renal Cell |
State University of New York at Buffalo |
June 1 2024 | Phase 1|Phase 2 |
| NCT06208748 | Not yet recruiting | Gastrointestinal Stromal Tumors|GIST |
Sarcoma Alliance for Research through Collaboration|Cogent Biosciences Inc.|Dana-Farber Cancer Institute|The Life Raft Group |
March 2024 | Phase 2 |
| NCT05745142 | Completed | Carcinoma Renal Cell|Clear-cell Metastatic Renal Cell Carcinoma |
Pfizer |
February 23 2023 | -- |
| NCT05043090 | Recruiting | Papillary Renal Cell Carcinoma |
AstraZeneca |
October 28 2021 | Phase 3 |
| NCT04669366 | Completed | Kidney Neoplasms |
Pfizer |
January 20 2021 | -- |
化学信息&溶解度
| 分子量 | 532.56 | 分子式 | C22H27FN4O2.C4H6O5 |
| CAS号 | 341031-54-7 | SDF | Download Sunitinib malate SDF |
| Smiles | CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 70 mg/mL ( (131.44 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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如果有其他问题，请给我们留言。
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常见问题及建议解决方法
问题 1:
I was wondering that the compound is in its cis or trans form?
回答：
S1042 Sunitinib Malate is Z form.
问题 2:
What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?
回答：
S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.
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