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Dasatinib Monohydrate
别名: BMS-354825 Monohydrate 中文名称：达沙替尼一水合物
Dasatinib Monohydrate (BMS-354825)是一种新型有效的多靶点抑制剂，作用于靶点Abl，Src 和 c-Kit，IC50分别为 <1 nM，0.8 nM 和 79 nM。
Dasatinib Monohydrate Chemical Structure
CAS: 863127-77-9
产品质控
批次：
纯度：
99.62%
99.62
Dasatinib Monohydrate相关产品
| 相关靶点 | Lck Fyn Lyn Yes Fgr | 点击展开 |
|---|---|---|
| 相关产品 | Saracatinib (AZD0530) PP2 SU6656 PP1 WH-4-023 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 Myristic Acid RK 24466 eCF506 | 点击展开 |
| 相关化合物库 | 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 血管生成相关化合物库 HIF-1信号通路化合物库 FDA抗癌药物库 | 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(PMID) |
|---|---|---|---|---|---|
| K562 cell | Proliferation assay | 72 h | Antiproliferative activity against human K562 cells after 72 hrs, IC50=0.001 μM | ||
| WiDr cell | Proliferation assay | 72 h | Antiproliferative activity against human WiDr cells after 72 hrs, IC50=0.052 μM | ||
| PC3 cell | Proliferation assay | 72 h | Antiproliferative activity against human PC3 cells after 72 hrs, IC50=0.0094 μM | ||
| MDA-MB-231 cell | Proliferation assay | 72 h | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs, IC50=0.012 μM | ||
| M07ep210 cell | Growth inhibition assay | 48 h | Growth inhibition of human M07ep210 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.07 nM | ||
| K562 cell | Growth inhibition assay | 48 h | Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.001 μM | ||
| M07e cell | Growth inhibition assay | 48 h | Growth inhibition of human M07e cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.0012 μM | ||
| K562 cell | Cytotoxicity assay | 72 h | Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=12.83 μM | ||
| U937 cell | Cytotoxicity assay | 72 h | Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=13.63 μM | ||
| K562 cell | Proliferation assay | 72 h | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50=0.7 nM | ||
| MDA-MB-435S cell | Proliferation assay | 72 h | Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50=3.9 μM | ||
| NCI-H460 cell | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50=8.99 μM | ||
| NCI-H23 cell | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50=2.27 μM | ||
| A549 cell | Proliferation assay | 72 h | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=12.66 μM | ||
| T47D cell | Proliferation assay | 72 h | Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50=0.9 μM | ||
| HCT116 cell | Proliferation assay | 72 h | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=2.3 μM | ||
| MCF7 cells | Proliferation assay | 72 h | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=2.57 μM | ||
| RXF 393NL cell | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining, IC50=21.7 nM | ||
| PRXF DU145 cell | Cytotoxicity assay | 4 days | Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining, IC50=0.0623 μM | ||
| LXFA 983L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 983L cells after 4 days by propidium iodide staining, IC50=56.5 nM | ||
| GXF251L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining, IC50=2.25 μM | ||
| CXF 1103L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human CXF 1103L cells after 4 days by propidium iodide staining, IC50=4.36 μM | ||
| PAXF 1657L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining, IC50=0.121 μM | ||
| NCI-H1648 cell | Growth inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.02011 μM | |||
| NCI-H1838 cell | Growth inhibition assay | Inhibition of human NCI-H1838 cell growth in a cell viability assay, IC50=1.30733 μM | |||
| NCI-H2126 cell | Growth inhibition assay | Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=2.87552 μM | |||
| NCI-H2141 cell | Growth inhibition assay | Inhibition of human NCI-H2141 cell growth in a cell viability assay, IC50=24.7754 μM | |||
| NCI-H2107 cell | Growth inhibition assay | Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=43.4847 μM | |||
| NCI-H747 cell | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=0.08362 μM | |||
| NCI-H720 cell | Growth inhibition assay | Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=20.2733 μM | |||
| NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay.IC50=1.30859 μM | |||
| NMC-G1 cell | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay.IC50=0.11606 μM | |||
| NTERA-S-cl-D1 cell | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay.IC50=0.12283 μM | |||
| OCI-AML2 cell | Growth inhibition assay | Inhibition of human OCI-AML2 cell growth in a cell viability assay.IC50=5.86154 μM | |||
| OCUB-M cell | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay.IC50=1.04412 μM | |||
| OPM-2 cell | Growth inhibition assay | Inhibition of human OPM-2 cell growth in a cell viability assay.IC50=4.27685 μM | |||
| OS-RC-2 cell | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay.IC50=0.0203 μM | |||
| ONS-76 cell | Growth inhibition assay | Inhibition of human ONS-76 cell growth in a cell viability assay.IC50=0.42951 μM | |||
| OVCAR-4 cell | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay.IC50=0.37433 μM | |||
| NCI-H446 cell | Growth inhibition assay | Inhibition of human NCI-H446 cell growth in a cell viability assay.IC50=0.6276 μM | |||
| NCI-H510A cell | Growth inhibition assay | Inhibition of human NCI-H510A cell growth in a cell viability assay.IC50=19.3973 μM | |||
| PF-382 cell | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay.IC50=0.17678 μM | |||
| NCI-H64 cell | Growth inhibition assay | Inhibition of human NCI-H64 cell growth in a cell viability assay.IC50=29.6253 μM | |||
| PSN1 cell | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay.IC50=0.04474 μM | |||
| QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay.IC50=0.70629 μM | |||
| RL95-2 cell | Growth inhibition assay | Inhibition of human RL95-2 cell growth in a cell viability assay.IC50=0.1038 μM | |||
| RCC10RGB cell | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay.IC50=0.4911 μM | |||
| RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay.IC50=0.52966 μM | |||
| NCI-SNU-16 cell | Growth inhibition assay | Inhibition of human NCI-SNU-16 cell growth in a cell viability assay.IC50=8.56128 μM | |||
| RPMI-6666 cell | Growth inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay.IC50=7.27067 μM | |||
| NEC8 cell | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay.IC50=44.336 μM | |||
| RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay.IC50=7.65787 μM | |||
| RXF393 cell | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay.IC50=0.02357 μM | |||
| Raji cell | Growth inhibition assay | Inhibition of human Raji cell growth in a cell viability assay.IC50=13.7497 μM | |||
| NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay.IC50=0.006129 μM | |||
| SBC-1 cell | Growth inhibition assay | Inhibition of human SBC-1 cell growth in a cell viability assay.IC50=1.57984 μM | |||
| SF126 cell | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay.IC50=0.3541 μM | |||
| SF539 cell | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay.IC50=13.8557 μM | |||
| SH-4 cell | Growth inhibition assay | Inhibition of human SH-4 cell growth in a cell viability assay.IC50=0.18413 μM | |||
| OMC-1 cell | Growth inhibition assay | Inhibition of human OMC-1 cell growth in a cell viability assay.IC50=27.1422 μM | |||
| SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay.IC50=9.02493 μM | |||
| SJSA-1 cell | Growth inhibition assay | Inhibition of human SJSA-1 cell growth in a cell viability assay.IC50=8.72805 μM | |||
| SK-LMS-1 cell | Growth inhibition assay | Inhibition of human SK-LMS-1 cell growth in a cell viability assay.IC50=3.11886 μM | |||
| SK-NEP-1 cell | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay.IC50=8.89155 μM | |||
| SKM-1 cell | Growth inhibition assay | Inhibition of human SKM-1 cell growth in a cell viability assay.IC50=9.01734 μM | |||
| SK-PN-DW cell | Growth inhibition assay | Inhibition of human SK-PN-DW cell growth in a cell viability assay.IC50=36.1943 μM | |||
| SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay.IC50=2.16693 μM | |||
| SNB75 cell | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay.IC50=0.04435 μM | |||
| REH cell | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay.IC50=20.6357 μM | |||
| SNU-C2B cell | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay.IC50=1.30589 μM | |||
| RPMI-8866 cell | Growth inhibition assay | Inhibition of human RPMI-8866 cell growth in a cell viability assay.IC50=17.4455 μM | |||
| SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay.IC50=0.04161 μM | |||
| SW962 cell | Growth inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay.IC50=0.11292 μM | |||
| SF268 cell | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay.IC50=0.17404 μM | |||
| TE-1 cell | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay.IC50=0.1054 μM | |||
| 8-MG-BA cell | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay.IC50=0.15458 μM | |||
| A101D cell | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay.IC50=1.03043 μM | |||
| A253 cell | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay.IC50=3.73246 μM | |||
| A3-KAW cell | Growth inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay.IC50=0.98452 μM | |||
| A4-Fuk cell | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay.IC50=38.1009 μM | |||
| A388 cell | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay.IC50=0.05095 μM | |||
| ACN cell | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay.IC50=1.82252 μM | |||
| A704 cell | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay.IC50=0.01491 μM | |||
| ALL-PO cell | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay.IC50=10.7938 μM | |||
| ARH-77 cell | Growth inhibition assay | Inhibition of human ARH-77 cell growth in a cell viability assay.IC50=3.46915 μM | |||
| SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay.IC50=4.49954 μM | |||
| BB65-RCC cell | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay.IC50=0.08227 μM | |||
| BB49-HNC cell | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay.IC50=0.38599 μM | |||
| BC-1 cell | Growth inhibition assay | Inhibition of human BC-1 cell growth in a cell viability assay.IC50=28.651 μM | |||
| BC-3 cell | Growth inhibition assay | Inhibition of human BC-3 cell growth in a cell viability assay.IC50=12.1138 μM | |||
| BL-41 cell | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay.IC50=0.29123 μM | |||
| BL-70 cell | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay.IC50=0.0000008218 μM | |||
| SW684 cell | Growth inhibition assay | Inhibition of human SW684 cell growth in a cell viability assay.IC50=0.3498 μM | |||
| BOKU cell | Growth inhibition assay | Inhibition of human BOKU cell growth in a cell viability assay.IC50=0.49133 μM | |||
| SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay.IC50=0.02927 μM | |||
| C2BBe1 cell | Growth inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay.IC50=0.08308 μM | |||
| BV-173 cell | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay.IC50=0.000000109 μM | |||
| Becker cell | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay.IC50=0.03003 μM | |||
| SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay.IC50=0.01115 μM | |||
| 697 cell | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay.IC50=0.19987 μM | |||
| TE-15 cell | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay.IC50=0.005891 μM | |||
| TE-11 cell | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay.IC50=0.07858 μM | |||
| TE-5 cell | Growth inhibition assay | Inhibition of human TE-5 cell growth in a cell viability assay.IC50=1.79139 μM | |||
| TE-6 cell | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay.IC50=1.21226 μM | |||
| TE-9 cell | Growth inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay.IC50=0.87532 μM | |||
| TGBC24TKB cell | Growth inhibition assay | Inhibition of human TGBC24TKB cell growth in a cell viability assay.IC50=0.04761 μM | |||
| TGW cell | Growth inhibition assay | Inhibition of human TGW cell growth in a cell viability assay.IC50=11.2828 μM | |||
| TK10 cell | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay.IC50=0.01174 μM | |||
| TGBC1TKB cell | Growth inhibition assay | Inhibition of human TGBC1TKB cell growth in a cell viability assay.IC50=0.06164 μM | |||
| A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay.IC50=0.07284 μM | |||
| UACC-257 cell | Growth inhibition assay | Inhibition of human UACC-257 cell growth in a cell viability assay.IC50=12.9198 μM | |||
| U-87-MG cell | Growth inhibition assay | Inhibition of human U-87-MG cell growth in a cell viability assay.IC50=30.766 μM | |||
| BB30-HNC cell | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay.IC50=0.05437 μM | |||
| no-10 cell | Growth inhibition assay | Inhibition of human no-10 cell growth in a cell viability assay.IC50=0.31931 μM | |||
| CAS-1 cell | Growth inhibition assay | Inhibition of human CAS-1 cell growth in a cell viability assay.IC50=1.40992 μM | |||
| CGTH-W-1 cell | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay.IC50=0.03548 μM | |||
| TE-10 cell | Growth inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay.IC50=0.06357 μM | |||
| COLO-684 cell | Growth inhibition assay | Inhibition of human COLO-684 cell growth in a cell viability assay.IC50=46.2258 μM | |||
| TE-12 cell | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay.IC50=0.01861 μM | |||
| COR-L279 cell | Growth inhibition assay | Inhibition of human COR-L279 cell growth in a cell viability assay.IC50=40.2852 μM | |||
| TE-8 cell | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay.IC50=0.01576 μM | |||
| CP66-MEL cell | Growth inhibition assay | Inhibition of human CP66-MEL cell growth in a cell viability assay.IC50=0.19531 μM | |||
| CTV-1 cell | Growth inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay.IC50=0.00004036 μM | |||
| VA-ES-BJ cell | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay.IC50=0.03902 μM | |||
| D-263MG cell | Growth inhibition assay | Inhibition of human D-263MG cell growth in a cell viability assay.IC50=0.36224 μM | |||
| D-336MG cell | Growth inhibition assay | Inhibition of human D-336MG cell growth in a cell viability assay.IC50=0.006298 μM | |||
| D-502MG cell | Growth inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay.IC50=1.23376 μM | |||
| DJM-1 cell | Growth inhibition assay | Inhibition of human DJM-1 cell growth in a cell viability assay.IC50=6.48558 μM | |||
| no-11 cell | Growth inhibition assay | Inhibition of human no-11 cell growth in a cell viability assay.IC50=0.50228 μM | |||
| DMS-153 cell | Growth inhibition assay | Inhibition of human DMS-153 cell growth in a cell viability assay.IC50=14.0028 μM | |||
| DSH1 cell | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay.IC50=0.24001 μM | |||
| DU-4475 cell | Growth inhibition assay | Inhibition of human DU-4475 cell growth in a cell viability assay.IC50=8.21652 μM | |||
| EB-3 cell | Growth inhibition assay | Inhibition of human EB-3 cell growth in a cell viability assay.IC50=34.3118 μM | |||
| EHEB cell | Growth inhibition assay | Inhibition of human EHEB cell growth in a cell viability assay.IC50=10.0656 μM | |||
| COLO-829 cell | Growth inhibition assay | Inhibition of human COLO-829 cell growth in a cell viability assay.IC50=0.12213 μM | |||
| CP67-MEL cell | Growth inhibition assay | Inhibition of human CP67-MEL cell growth in a cell viability assay.IC50=0.20488 μM | |||
| ES8 cell | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay.IC50=32.1252 μM | |||
| EVSA-T cell | Growth inhibition assay | Inhibition of human EVSA-T cell growth in a cell viability assay.IC50=9.27793 μM | |||
| ES4 cell | Growth inhibition assay | Inhibition of human ES4 cell growth in a cell viability assay.IC50=1.05145 μM | |||
| ETK-1 cell | Growth inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay.IC50=0.02832 μM | |||
| ES6 cell | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay.IC50=0.03193 μM | |||
| EW-24 cell | Growth inhibition assay | Inhibition of human EW-24 cell growth in a cell viability assay.IC50=0.78165 μM | |||
| EoL-1-cell cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay.IC50=0.00001309 μM | |||
| Calu-6 cell | Growth inhibition assay | Inhibition of human Calu-6 cell growth in a cell viability assay.IC50=3.05741 μM | |||
| GAK cell | Growth inhibition assay | Inhibition of human GAK cell growth in a cell viability assay.IC50=31.2686 μM | |||
| D-247MG cell | Growth inhibition assay | Inhibition of human D-247MG cell growth in a cell viability assay.IC50=6.12519 μM | |||
| GB-1 cell | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay.IC50=0.02157 μM | |||
| GI-ME-N cell | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay.IC50=0.06118 μM | |||
| GCIY cell | Growth inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay.IC50=0.09656 μM | |||
| GT3TKB cell | Growth inhibition assay | Inhibition of human GT3TKB cell growth in a cell viability assay.IC50=9.35546 μM | |||
| HC-1 cell | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay.IC50=24.5551 μM | |||
| HAL-01 cell | Growth inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay.IC50=19.7543 μM | |||
| HCC1187 cell | Growth inhibition assay | Inhibition of human HCC1187 cell growth in a cell viability assay.IC50=35.8052 μM | |||
| DEL cell | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay.IC50=41.9086 μM | |||
| HCC1599 cell | Growth inhibition assay | Inhibition of human HCC1599 cell growth in a cell viability assay.IC50=32.3325 μM | |||
| DOHH-2 cell | Growth inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay.IC50=0.01719 μM | |||
| HCC2157 cell | Growth inhibition assay | Inhibition of human HCC2157 cell growth in a cell viability assay.IC50=37.9946 μM | |||
| HCE-4 cell | Growth inhibition assay | Inhibition of human HCE-4 cell growth in a cell viability assay.IC50=0.26439 μM | |||
| HCE-T cell | Growth inhibition assay | Inhibition of human HCE-T cell growth in a cell viability assay.IC50=1.56714 μM | |||
| HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay.IC50=10.4776 μM | |||
| EM-2 cell | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay.IC50=0.000001078 μM | |||
| HT-144 cell | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay.IC50=0.53609 μM | |||
| EW-16 cell | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay.IC50=0.76178 μM | |||
| IA-LM cell | Growth inhibition assay | Inhibition of human IA-LM cell growth in a cell viability assay.IC50=12.4445 μM | |||
| IST-MEL1 cell | Growth inhibition assay | Inhibition of human IST-MEL1 cell growth in a cell viability assay.IC50=0.1345 μM | |||
| IST-MES1 cell | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay.IC50=0.08552 μM | |||
| GI-1 cell | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay.IC50=1.3622 μM | |||
| IST-SL2 cell | Growth inhibition assay | Inhibition of human IST-SL2 cell growth in a cell viability assay.IC50=0.50302 μM | |||
| JVM-2 cell | Growth inhibition assay | Inhibition of human JVM-2 cell growth in a cell viability assay.IC50=2.36284 μM | |||
| JVM-3 cell | Growth inhibition assay | Inhibition of human JVM-3 cell growth in a cell viability assay.IC50=37.2338 μM | |||
| KALS-1 cell | Growth inhibition assay | Inhibition of human KALS-1 cell growth in a cell viability assay.IC50=0.0949 μM | |||
| KARPAS-422 cell | Growth inhibition assay | Inhibition of human KARPAS-422 cell growth in a cell viability assay.IC50=0.33997 μM | |||
| JiyoyeP-2003 cell | Growth inhibition assay | Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay.IC50=1.73466 μM | |||
| KARPAS-45 cell | Growth inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay.IC50=7.51671 μM | |||
| KGN cell | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay.IC50=0.01942 μM | |||
| KLE cell | Growth inhibition assay | Inhibition of human KLE cell growth in a cell viability assay.IC50=0.11317 μM | |||
| KNS-42 cell | Growth inhibition assay | Inhibition of human KNS-42 cell growth in a cell viability assay.IC50=1.24412 μM | |||
| KNS-81-FD cell | Growth inhibition assay | Inhibition of human KNS-81-FD cell growth in a cell viability assay.IC50=23.146 μM | |||
| KP-N-YS cell | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay.IC50=12.9283 μM | |||
| HOP-62 cell | Growth inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay.IC50=0.01834 μM | |||
| KURAMOCHI cell | Growth inhibition assay | Inhibition of human KURAMOCHI cell growth in a cell viability assay.IC50=0.03487 μM | |||
| HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay.IC50=0.3142 μM | |||
| LAMA-84 cell | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay.IC50=0.000003207 μM | |||
| LB1047-RCC cell | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay.IC50=0.009887 μM | |||
| LB2518-MEL cell | Growth inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay.IC50=0.14162 μM | |||
| LB373-MEL-D cell | Growth inhibition assay | Inhibition of human LB373-MEL-D cell growth in a cell viability assay.IC50=0.82508 μM | |||
| LB771-HNC cell | Growth inhibition assay | Inhibition of human LB771-HNC cell growth in a cell viability assay.IC50=2.57551 μM | |||
| LB996-RCC cell | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay.IC50=0.009912 μM | |||
| LC-2-ad cell | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay.IC50=0.02586 μM | |||
| J-RT3-T3-5 cell | Growth inhibition assay | Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay.IC50=8.96529 μM | |||
| LP-1 cell | Growth inhibition assay | Inhibition of human LP-1 cell growth in a cell viability assay.IC50=7.54782 μM | |||
| K-562 cell | Growth inhibition assay | Inhibition of human K-562 cell growth in a cell viability assay.IC50=0.0000002656 μM | |||
| LS-123 cell | Growth inhibition assay | Inhibition of human LS-123 cell growth in a cell viability assay.IC50=0.14064 μM | |||
| K5 cell | Growth inhibition assay | Inhibition of human K5 cell growth in a cell viability assay.IC50=0.16489 μM | |||
| LS-411N cell | Growth inhibition assay | Inhibition of human LS-411N cell growth in a cell viability assay.IC50=48.4748 μM | |||
| KG-1 cell | Growth inhibition assay | Inhibition of human KG-1 cell growth in a cell viability assay.IC50=4.60845 μM | |||
| KINGS-1 cell | Growth inhibition assay | Inhibition of human KINGS-1 cell growth in a cell viability assay.IC50=0.16666 μM | |||
| LXF-289 cell | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay.IC50=0.03956 μM | |||
| MC116 cell | Growth inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay.IC50=0.1141 μM | |||
| KS-1 cell | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay.IC50=0.0273 μM | |||
| KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay.IC50=0.11883 μM | |||
| MEG-01 cell | Growth inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay.IC50=0.000009805 μM | |||
| MFH-ino cell | Growth inhibition assay | Inhibition of human MFH-ino cell growth in a cell viability assay.IC50=0.04724 μM | |||
| L-540 cell | Growth inhibition assay | Inhibition of human L-540 cell growth in a cell viability assay.IC50=15.0671 μM | |||
| MHH-NB-11 cell | Growth inhibition assay | Inhibition of human MHH-NB-11 cell growth in a cell viability assay.IC50=43.0818 μM | |||
| MMAC-SF cell | Growth inhibition assay | Inhibition of human MMAC-SF cell growth in a cell viability assay.IC50=8.79307 μM | |||
| LB2241-RCC cell | Growth inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay.IC50=9.02012 μM | |||
| LB831-BLC cell | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay.IC50=0.04609 μM | |||
| MOLT-16 cell | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay.IC50=29.6292 μM | |||
| LC-1F cell | Growth inhibition assay | Inhibition of human LC-1F cell growth in a cell viability assay.IC50=27.3245 μM | |||
| MOLT-4 cell | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay.IC50=26.6753 μM | |||
| MZ1-PC cell | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay.IC50=0.03119 μM | |||
| MONO-MAC-6 cell | Growth inhibition assay | Inhibition of human MONO-MAC-6 cell growth in a cell viability assay.IC50=8.27066 μM | |||
| MZ2-MEL cell | Growth inhibition assay | Inhibition of human MZ2-MEL cell growth in a cell viability assay.IC50=0.28537 μM | |||
| MPP-89 cell | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay.IC50=0.04049 μM | |||
| MZ7-mel cell | Growth inhibition assay | Inhibition of human MZ7-mel cell growth in a cell viability assay.IC50=0.47911 μM | |||
| LOXIMVI cell | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay.IC50=0.31503 μM | |||
| NALM-6 cell | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay.IC50=0.19295 μM | |||
| NB13 cell | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay.IC50=19.4877 μM | |||
| NB5 cell | Growth inhibition assay | Inhibition of human NB5 cell growth in a cell viability assay.IC50=1.39827 μM | |||
| NB17 cell | Growth inhibition assay | Inhibition of human NB17 cell growth in a cell viability assay.IC50=3.63847 μM | |||
| NCCIT cell | Growth inhibition assay | Inhibition of human NCCIT cell growth in a cell viability assay.IC50=2.86616 μM | |||
| NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay.IC50=0.14436 μM | |||
| NCI-H1304 cell | Growth inhibition assay | Inhibition of human NCI-H1304 cell growth in a cell viability assay.IC50=28.1628 μM | |||
| NCI-H1395 cell | Growth inhibition assay | Inhibition of human NCI-H1395 cell growth in a cell viability assay.IC50=42.0163 μM | |||
| MHH-PREB-1 cell | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay.IC50=0.74469 μM | |||
| MLMA cell | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay.IC50=0.14032 μM | |||
| MN-60 cell | Growth inhibition assay | Inhibition of human MN-60 cell growth in a cell viability assay.IC50=15.1979 μM | |||
| MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay.IC50=4.36454 μM | |||
| NB6 cell | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay.IC50=9.92259 μM | |||
| NCI-H1355 cell | Growth inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay.IC50=0.11028 μM | |||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Dasatinib Monohydrate (BMS-354825)是一种新型有效的多靶点抑制剂，作用于靶点Abl，Src 和 c-Kit，IC50分别为 <1 nM，0.8 nM 和 79 nM。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Dasatinib比imatinib更有效地抑制表达野生型Bcr-Abl 和Bcr-Abl突变体的Ba/F3细胞的增殖，T315I突变体除外。相对于imatinib，Dasatinib具有双对数(∼325倍)增加的效能。Dasatinib有效抑制野生型Abl激酶和除T315I外小范围的所有突变体。Dasatinib直接靶向作用于所有突变型Abl激酶域，并以浓度依赖的方式抑制自身磷酸化和底物磷酸化。与imatinib相比，Dasatinib对表达野生型Bcr-Abl的细胞表现出325倍的效能。[1] TgE骨髓细胞集落百分数在未处理的孔中为100%，在Dasatinib处理的孔中降低为4.12%。在Dasatinib存在下，WT和TgE骨髓细胞形成的集落百分比在统计学上具有显著差异。LMP2A的表达能够促进B淋巴细胞存活和增殖，这能够被以Lyn 和/或c-Abl激酶为靶点的Dasatinib抑制。[3] Dasatinib治疗抑制一部分甲状腺癌细胞中Src信号，减少生长，并诱导细胞周期阻滞和细胞凋亡。以逐渐增加剂量的纳摩尔级浓度的Dasatinib (0.019 μM到1.25 μM)治疗3天，抑制大约50%的C643，TPC1，BCPAP，和SW1736细胞系生长，而抑制K1细胞系的生长需要更高浓度。10 nM 或50 nM Dasatinib治疗导致BCPAP ，SW1736和 K1细胞中G1期细胞增加9-22%，而S期细胞相应减少7-18%。[4] | |||
|---|---|---|---|---|
| 激酶实验 | 激酶自磷酸化测定 | |||
| 激酶试验使用野生型和突变型谷胱甘肽S转移酶(GST)-Abl融合蛋白(c-Abl 氨基酸220-498)进行。GST-Abl在使用前从谷胱甘肽-琼脂糖珠中释放；ATP浓度为5 μM。在用于激酶磷酸化和体外多肽底物磷酸化试验之前，GST-Abl激酶域融合蛋白立即用LAR酪氨酸磷酸酶处理。在30℃下培养1小时后，LAR磷酸酶通过加入钒酸钠(1 mM)灭活。比较未处理的GST-Abl激酶和去磷酸化的GST-Abl激酶，免疫印记分析按照常规进行，使用磷酸酪氨酸特异性抗体4G10以确定酪氨酸残基完全去磷酸化(>95%)，使用c-Abl抗体CST 2862确定GST-Abl激酶等量加入。对于突变型T315I，Dasatinib浓度范围扩展到1,000 nM。这些同样的抑制剂浓度用于体外多肽底物磷酸化试验。测试三个抑制剂在相同浓度范围内对GST-Src 激酶和GST-Lyn激酶的抑制作用。 | ||||
| 细胞实验 | 细胞系 | Ba/F3 细胞系 | ||
| 浓度 | ~32 nM | |||
| 孵育时间 | 72小时 | |||
| 方法 | Ba/F3细胞系以一式三份接种，并与逐渐增加浓度的Dasatinib培养72小时。使用基于甲烷硫代磺酸盐的活性试验测量增殖。IC50和IC90值以重复四次的三个独立实验平均值确定。抑制剂浓度范围为0 nM到32 nM (Dasatinib)。对于突变型T315I，Dasatinib浓度范围扩展到200 nM。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 cleaved caspase 3 p-FAK/p-STAT3 |
|
23049975 | |
| Growth inhibition assay | Cell viability |
|
23721490 | |
| Immunofluorescence | SRC / Met α-tubulin F-actin / Actinin-4 / Paxillin |
|
26517812 | |
| ELISA | TNF-α E-selectin VCAM-1 |
|
17684099 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Dasatinib逆转LMP2A/MYC双重转基因小鼠体内的脾肿大。在TgE 小鼠体内，Dasatinib特异性防止LMP2A表达的骨髓B细胞形成集落，并减少脾脏大小。与对照组相比，Dasatinib治疗的Tg6/λ-MYC小鼠中，脾脏肿块显著减小。Dasatinib抑制LMP2A/MYC双重转基因小鼠体内的淋巴结肿大。从LMP2A/MYC双重转基因小鼠移植肿瘤细胞的Rag1KO小鼠体内，Dasatinib逆转脾肿大。Dasatinib治疗抑制表达LMP2A的B淋巴肿瘤细胞中Lyn磷酸化。[3] | |
|---|---|---|
| 动物实验 | Animal Models | EμLMP2A (TgE和Tg6菌株)，MYC (λ-MYC)，和LMP2A/λ-MYC 双重转基因小鼠(Tg6/λ-MYC) |
| Dosages | 30 mg/kg | |
| Administration | 腹腔注射给药 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05527418 | Recruiting | Recent HIV-1 Infection |
Eva Bonfill|Institut d''Investigacions Biomèdiques August Pi i Sunyer |
January 26 2024 | Phase 2 |
| NCT05993949 | Recruiting | Lymphoblastic Leukemia |
Stanford University|Kite Pharma |
October 2 2023 | Phase 1 |
| NCT05780073 | Recruiting | HIV Infection Primary |
Fundació Institut Germans Trias i Pujol|Fundación FLS de Lucha Contra el Sida Enfermedades Infecciosas y Promoción de la Salud y Ciencia|Spanish Clinical Research Network - SCReN|IrsiCaixa|University of Turin Italy|Instituto de Salud Carlos III|Germans Trias i Pujol Hospital |
October 16 2023 | Phase 2 |
| NCT05198843 | Terminated | Anatomic Stage IV Breast Cancer AJCC v8|Metastatic Triple-Negative Breast Inflammatory Carcinoma |
National Cancer Institute (NCI) |
November 8 2022 | Phase 1|Phase 2 |
| NCT04925648 | Recruiting | Metastatic Prostate Cancer |
St Vincent''s Hospital Sydney |
October 18 2021 | Phase 2 |
|
化学信息&溶解度
| 分子量 | 506.02 | 分子式 | C22H28ClN7O3S |
| CAS号 | 863127-77-9 | SDF | Download Dasatinib Monohydrate SDF |
| Smiles | CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.O | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (197.62 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 |
|
体内溶解配方 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。
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常见问题及建议解决方法
问题 1:
What’s the difference between S1021 and S7782?
回答：
Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than hydrate one (S7782).
