Foretinib

别名: GSK1363089, EXEL-2880, XL-880, GSK089

目录号：S1111 Purity: 99.82%

Foretinib是一种ATP竞争性的HGFR和VEGFR抑制剂，对Met (c-Met)和KDR作用最强，在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron， Flt-1/3/4， Kit (c-Kit)， PDGFRα/β和Tie-2作用效果稍弱，对FGFR1和EGFR几乎没有抑制活性。Phase 2。

Foretinib Chemical Structure

CAS: 849217-64-7

规格	价格	库存
10mM (1mL in DMSO)	2340.27	现货
5mg	1374.78	现货
50mg	7124.95	现货
1g	24488.1	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次： S111106 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false 纯度： 99.82%

99.82

Foretinib相关产品

相关产品	SGX-523 PHA-665752 SU11274 BMS-777607 JNJ-38877605 Tivantinib PF-04217903 Tepotinib Savolitinib (AZD6094) MGCD-265 analog Golvatinib (E7050) Merestinib (LY2801653) MK-2461 NPS-1034 AMG 337 Sodium L-ascorbyl-2-phosphate NVP-BVU972 BMS-794833 S49076	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

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	Function Assay	100/300/900 nM	24 h	abrogates migration and invasion of glioma cells in a dose dependent manner	24658326
SF188	Function Assay	100/300/900 nM	24 h	abrogates migration and invasion of glioma cells in a dose dependent manner	24658326
A172	Growth Inhibition Assay	100/300/900 nM	48 h	reduces cell survival at 900 nM significantly	24658326
U251	Growth Inhibition Assay	100/300/900 nM	48 h	reduces cell survival at 900 nM significantly	24658326
SF188	Growth Inhibition Assay	100/300/900 nM	48 h	reduces cell survival at 900 nM significantly	24658326
SF188	Function Assay	100/300/900 nM	28 h	induces PARP cleavage	24658326
U251	Function Assay	100/300/900 nM	28 h	induces PARP cleavage	24658326
SF188	Function Assay	100/300/900 nM	1 h	decreases Akt phosphorylation in a concentration dependent manner	24658326
A172	Function Assay	100/300/900 nM	1 h	decreases Akt phosphorylation in a concentration dependent manner	24658326
U251	Function Assay	100/300/900 nM	1 h	decreases Akt phosphorylation in a concentration dependent manner	24658326
SF188	Function Assay	100/300/900 nM	1 h	inhibits the activity of Axl, Tyro3	24658326
A172	Function Assay	100/300/900 nM	1 h	inhibits the activity of Axl, Tyro3	24658326
U251	Function Assay	100/300/900 nM	1 h	inhibits the activity of Axl, Tyro3	24658326
SF188	Function Assay	100/300/900 nM	1 h	inhibits the phosphorylation of MerTK	24658326
A172	Function Assay	100/300/900 nM	1 h	inhibits the phosphorylation of MerTK	24658326
U251	Function Assay	100/300/900 nM	1 h	inhibits the phosphorylation of MerTK	24658326
Daoy	Growth Inhibition Assay	0.5/1/2.5 μM	24-96 h	inhibits cell growth in a dose dependent manner	25391241
Daoy	Apoptosis Assay	1 μM	24 h	induces apoptosis	25391241
ONS76	Function Assay	0.5/1/2.5 μM	24 h	inhibits HGF-mediated migration and invasion	25391241
Daoy	Function Assay	0.5/1/2.5 μM	24 h	inhibits HGF-mediated migration and invasion	25391241
ONS76	Function Assay	0.5/1/2.5 μM	24 h	inhibits the HGF-induced cMET pathway activation	25391241
Daoy	Function Assay	0.5/1/2.5 μM	24 h	inhibits the HGF-induced cMET pathway activation	25391241
A172	Function Assay	100/300/900 nM	24 h	abrogates migration and invasion of glioma cells in a dose dependent manner	24658326
Ba/F3	Cell Viability Assay	0.0001-10 μM	72 h	inhibits cell growth in a dose dependent manner	24218589
HCC78	Cell Viability Assay	0.01-10 μM	72 h	inhibits cell growth in a dose dependent manner	24218589
SK-HEP1	Cell Viability Assay	0.25-1.5 μM	24 h	inhibits cell growth in a dose dependent manner	22187171
SK-HEP2	Function Assay	1 μM	24 h	blocks HGF-induced cell motility	22187171
SK-HEP2	Function Assay	1 μM	24 h	causes G2/M phase arrest with reduction in the G0/G1 and S phases	22187171
MKN-45	Growth Inhibition Assay	0.01-10 μM	5 d	IC50=8 nM	21655918
KATO-III	Growth Inhibition Assay	0.01-10 μM	5 d	IC50=30 nM	21655918
MKN-45	Function Assay	1 μM	24 h	inhibits phosphorylation of MET, Akt, and ERK1/2 in MKN-45	21655918
KATO-III	Function Assay	1 μM	24 h	inhibits phosphorylation of MET, Akt, and ERK1/2 in MKN-45	21655918
HCC827	Apoptosis assay	0.01 to 1 uM	72 hrs	Induction of apoptosis in gefitinib resistant human HCC827 cells at 0.01 to 1 uM after 72 hrs by annexin V-FITC-propidium iodide staining-based flow cytometry method relative to control	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs	Inhibition of MET phosphorylation at Tyr1234/1235 in gefitinib resistant human HCC827 cells at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs	Downregulation of SMO expression in gefitinib resistant human HCC827 cells at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs	Inhibition of MET in gefitinib resistant human HCC827 cells assessed as decrease in MAPK44/42 phosphorylation at Thr202/Tyr204 at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs	Inhibition of MET in gefitinib resistant human HCC827 cells assessed as decrease in AKT phosphorylation at Ser473 at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs	Inhibition of MET/SMO V404M mutant in gefitinib resistant human HCC827 cells assessed as decrease in vimentin expression at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
NCI-H1993	Function assay	1 uM	4 hrs	Inhibition of c-MET D1228V mutant in CRISPR/Cas9 modified human NCI-H1993 cells assessed as reduction in AKT phosphorylation at 1 uM after 4 hrs by Western blot analysis	31531204
NCI-H1993	Function assay	1 uM	4 hrs	Inhibition of c-Met phosphorylation in human NCI-H1993 cells at 1 uM after 4 hrs by Western blot analysis	31531204
NCI-1993	Function assay	1 uM	4 hrs	Inhibition of c-MET in human NCI-1993 cells assessed as reduction in AKT phosphorylation at 1 uM after 4 hrs by Western blot analysis	31531204
NCI-H1993	Function assay	1 uM	4 hrs	Inhibition of c-Met D1228V mutant phosphorylation in CRISPR/Cas9 modified human NCI-H1993 cells at 1 uM after 4 hrs by Western blot analysis	31531204
HCC827	Antiproliferative assay	72 hrs		Antiproliferative activity against gefitinib resistant EGFR-mutated human HCC827 cells after 72 hrs by MTT assay, IC50 = 0.5 μM.	28787156
HCC827	Antitumor assay	15 mg/kg		Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 15 mg/kg/day, po	28787156
HCC827	Antitumor assay	20 mg/kg		Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po	28787156
HCC827	Antitumor assay	20 mg/kg		Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po in presence of gefitinib	28787156
HCC827	Antitumor assay	20 mg/kg		Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po in presence of osimertinib	28787156
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met-dependent human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.03 μM.	23628470
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met-dependent human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.08 μM.	23628470
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met-dependent human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.15 μM.	23628470
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met-independent human H460 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.18 μM.	23628470
SMMC7721	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met-dependent human SMMC7721 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.44 μM.	23628470
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met-dependent human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.9 μM.	23628470
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.031 μM.	23644189
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.12 μM.	23644189
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.18 μM.	23644189
SMMC7721	Cytotoxicity assay		72 hrs	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50 = 0.3 μM.	23644189
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.04 μM.	23644189
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM.	23838381
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by DAPI staining-based fluorescence assay, IC50 = 0.029 μM.	23838381
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by DAPI staining-based fluorescence assay, IC50 = 0.165 μM.	23838381
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.17 μM.	23838381
NCI-H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	23838381
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	23838381
SMMC7721	Cytotoxicity assay		72 hrs	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	23838381
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.47 μM.	23838381
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	24012712
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.11 μM.	24012712
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	24012712
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	24012712
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.08 μM.	24012712
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	24485123
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.13 μM.	24485123
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.16 μM.	24485123
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	24485123
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.1 μM.	24485123
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	24882675
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	24882675
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	24882675
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 0.54 μM.	24882675
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.032 μM.	24996144
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.11 μM.	24996144
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.19 μM.	24996144
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.21 μM.	24996144
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.08 μM.	24996144
MKN45	Antiproliferative assay		72 hrs	Antiproliferative activity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.032 μM.	25282672
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.12 μM.	25282672
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.19 μM.	25282672
H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.21 μM.	25282672
U87MG	Antiproliferative assay		72 hrs	Antiproliferative activity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.02 μM.	25282672
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	25438768
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.13 μM.	25438768
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.16 μM.	25438768
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	25438768
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.92 μM.	25438768
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.032 μM.	26169763
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.12 μM.	26169763
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.19 μM.	26169763
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.21 μM.	26169763
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM.	26810712
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM.	26810712
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM.	26810712
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM.	26897090
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.17 μM.	26897090
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	26897090
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.26 μM.	26923692
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.49 μM.	26923692
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.89 μM.	26923692
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 6.25 μM.	26923692
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.032 μM.	26944614
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.13 μM.	26944614
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.16 μM.	26944614
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.19 μM.	26944614
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 1.1 μM.	26944614
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM.	26964675
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM.	26964675
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM.	26964675
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay, IC50 = 0.0092 μM.	27068889
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells measured after 72 hrs by MTT assay, IC50 = 0.032 μM.	27155466
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells measured after 72 hrs by MTT assay, IC50 = 0.11 μM.	27155466
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells measured after 72 hrs by MTT assay, IC50 = 0.19 μM.	27155466
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells measured after 72 hrs by MTT assay, IC50 = 0.21 μM.	27155466
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM.	27187857
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.17 μM.	27187857
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	27187857
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 0.54 μM.	27187857
Sf9	Function assay		60 mins	Inhibition of NH2-terminal His-tagged MET kinase domain (1051 to 1348 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells preincubated for 60 mins followed by (poly(Glu, Tyr) 4:1) substrate addition for 2 to 4 hrs by luciferase-c, IC50 = 0.0004 μM.	27299736
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met over-expressed human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.032 μM.	27490023
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met over-expressed human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.14 μM.	27490023
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met over-expressed human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.19 μM.	27490023
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against c-Met over-expressed human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.21 μM.	27490023
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.15 μM.	28011202
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.25 μM.	28011202
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	28011202
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.25 μM.	28384549
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.29 μM.	28384549
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.36 μM.	28384549
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.96 μM.	28384549
MKN45	Antiproliferative assay		72 hrs	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.03 μM.	28716639
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.15 μM.	28716639
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	28716639
H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.22 μM.	28716639
U87MG	Antiproliferative assay		72 hrs	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.96 μM.	28716639
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.48 μM.	29107421
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.74 μM.	29107421
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.88 μM.	29107421
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 3.92 μM.	29107421
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	29197731
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.28 μM.	29197731
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	29197731
U87MG	Antiproliferative assay		72 hrs	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.91 μM.	29197731
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 2.27 μM.	29203143
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.76 μM.	29203143
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 3.13 μM.	29203143
PC3	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM.	29331754
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM.	29331754
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM.	29331754
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	30216852
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 0.48 μM.	30216852
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.76 μM.	30216852
MKN45	Antiproliferative assay		72 hrs	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.0023 μM.	30248654
EBC1	Antiproliferative assay		72 hrs	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0048 μM.	30248654
SNU5	Antiproliferative assay		72 hrs	Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay, IC50 = 0.0089 μM.	30248654
BAF3	Function assay		72 hrs	Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.0092 μM.	30248654
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.0396 μM.	30248654
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity in human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.041 μM.	31079967
NCI-H460	Cytotoxicity assay		72 hrs	Cytotoxicity in human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.18 μM.	31079967
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.22 μM.	31079967
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.52 μM.	31079967
sf21	Function assay		60 mins	Inhibition of wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay, IC50 = 0.002512 μM.	31531204
sf21	Function assay		60 mins	Inhibition of N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay, IC50 = 0.002512 μM.	31531204
NCI-H1993	Growth inhibition assay		3 days	Growth inhibition of CRISPR/Cas9 modified human NCI-H1993 cells harboring cMET D1228V mutant incubated for 3 days by cell titer-glo luminescent cell viability assay, GI50 = 0.05248 μM.	31531204
NCI-H1993	Growth inhibition assay		3 days	Growth inhibition of wild type human NCI-H1993 cells incubated for 3 days by cell titer-glo luminescent cell viability assay, GI50 = 0.06166 μM.	31531204
NCI-H1993	Function assay		4 hrs	Inhibition of c-Met phosphorylation at Tyr 1234/Tyr1235 residues in human NCI-H1993 cells incubated for 4 hrs by HTRF assay, IC50 = 0.2138 μM.	31531204
NCI-H1993	Function assay		4 hrs	Inhibition of c-MET D1228V mutant phosphorylation at Tyr1234/Tyr1235 residues in CRISPR/Cas9 modified human NCI-H1993 cells incubated for 4 hrs by HTRF assay, IC50 = 0.2138 μM.	31531204
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM.	31546197
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM.	31546197
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM.	31546197
MKN45	Cytotoxicity assay		72 hrs	Cytotoxicity against human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.2 μM.	31629631
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.14 μM.	31629631
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.49 μM.	31629631
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.76 μM.	31629631
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 2.17 μM.	31629631
H1648	Growth Inhibition Assay			IC50=1.28 ±0.12 μM	21252284
H1573	Growth Inhibition Assay			IC50=1.62 ± 0.05 μM	21252284
H596	Growth Inhibition Assay			IC50=1.21 ± 0.17 μM	21252284
HOP92	Growth Inhibition Assay			IC50=0.81 ± 0.29 μM	21252284
H69	Growth Inhibition Assay			IC50=1.18 ± 0.08 μM	21252284
H1975	Growth Inhibition Assay			IC50=1.39 ± 0.33 μM	21252284
SCC15	Growth Inhibition Assay			IC50=0.63 ± 0.04 μM	21252284
HN5	Growth Inhibition Assay			IC50=0.65 ± 0.26 μM	21252284
MKN45	Cytotoxicity assay			Cytotoxicity against human MKN45 cells, IC50 = 0.008 μM.	23838381
BA/F3	Function assay			Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells, IC50 = 0.01 μM.	25461320
BT474	Function assay			Inhibition of AXL in lapatinib-sensitive human BT474 cells, IC50 = 0.1 μM.	26555154
MKN45	Cytotoxicity assay			Cytotoxicity against human MKN45 cells, IC50 = 0.008 μM.	27187857
HT-29	Cytotoxicity assay			Cytotoxicity against human HT-29 cells, IC50 = 0.029 μM.	27187857
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells, IC50 = 0.165 μM.	27187857
HCC827	Function assay			Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting, Ki = 0.0668 μM.	28787156
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
sf21	Function assay			Binding affinity to wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 to 1390 residues) (unknown origin) expressed in sf21 cells by SPR analysis	31531204
sf21	Function assay			Binding affinity to N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells by SPR analysis	31531204
点击查看更多细胞系数据

生物活性

产品描述

靶点

Met ^[1] (Cell-free assay)	KDR ^[1] (Cell-free assay)	Tie-2 ^[1] (Cell-free assay)	VEGFR3/FLT4 ^[1] (Cell-free assay)	RON ^[1] (Cell-free assay)	点击更多
0.4 nM	0.86 nM	1.1 nM	2.8 nM	3 nM	点击更多

体外研究(In Vitro)
体外研究活性	XL880抑制HGF受体家族酪氨酸激酶，对Met和Ron 的IC50 值分别为0.4 nM和3 nM。XL880也会抑制KDR，Flt-1，和Flt-4，IC50值分别为0.9 nM，6.8 nM和2.8 nM。XL880抑制B16F10，A549 和HT29细胞集落生长，IC50分别为40 nM，29 nM和165 nM。^[1]一项最近的研究表明，XL880差异性影响胃癌细胞系MKN-45和KATO-III的细胞生长。XL880抑制MKN-45细胞中MET和下游信号分子的磷酸化，而在KATO-III细胞中靶向作用于GFGR2。^[2]
激酶实验	激酶抑制试验
激酶实验	激酶抑制使用三种测定形式中的一种进行研究：[³³P]磷酰基转移法，荧光素酶耦合的化学发光法，或AlphaScreen酪氨酸激酶技术。IC50s使用XLFit通过非线性回归分析计算。³³P-磷酰基转移激酶实验反应在384孔白色，透明底，高结合力微量滴定板(Greiner，Monroe，NC)中进行。板用50 μL体积的涂层缓冲液中的2 μg/well蛋白质或多肽底物涂覆，涂层缓冲液包含40 μg/mL底物(poly(Glu, Tyr) 4:1，22.5 mM Na2CO₃，27.5 mM NaHCO₃，50 mM NaCl 和3 mM NaN ₃。涂层的板用50 μL实验缓冲液洗涤一次，然后在室温下(RT)过夜培养。测试化合物和酶与³³P-γ-ATP (3.3 μCi/nmol)结合，总体积为20 μL。反应混合物在室温下培养2小时，然后通过抽吸终止。随后微量滴定板用0.05% Tween-PBS缓冲液(PBST)清洗6次。加入闪烁液(50 μL/well)，整合的³³P使用MicroBeta闪烁计数器通过液体闪烁光谱法测量。荧光素酶耦合的化学发光反应在384孔白色，含培养基的微量滴定板(Greiner)中进行。第一步，酶和化合物结合，并培养60分钟；加入终体积为20 μL的ATP与多肽底物(poly(Glu, Tyr) 4:1)起始反应，在室温下培养2-4小时。接下来进行激酶反应，加入20 μL等分激酶Glo (Promega，Madison，WI)，荧光信号使用Victor酶标仪测量。总ATP消耗限制在50%。AlphaScreenTM酪氨酸激酶测定使用链霉亲和素涂覆的供体珠和PY100抗磷酸酪氨酸抗体涂覆的受体珠进行。生物素化的聚(Glu,Tyr) 4:1用作底物。通过加入供体/受体珠，随后形成供体/受体珠复合物产生荧光测量底物磷酸化。激酶与测试化合物结合，并预培养60分钟，随后加入总体积为20 μL 的ATP，和生物素化的聚(Glu, Tyr)在384孔白色，含培养基的微量滴定板(Greiner)中。反应混合物在室温下培养1小时。然后加入包含75 mM Hepes，pH 7.4，300 mM NaCl，120 mM EDTA，0.3% BSA和0.03% Tween-20的10 μL 15-30 μg/mL AlphaScreen 珠悬浮液淬灭反应。室温下培养2-16小时后，板使用AlphaQuest阅读器读取数据。
细胞实验	细胞系	B16F10，A549，和 HT29 细胞
	浓度	40 nM
	孵育时间	12 到 14 天
	方法	B16F10，A549，和HT29细胞(1.2×10³/孔)与软琼脂混合，并接种于包含超过琼脂层的10% FBS 和EXEL-2880的96孔板。对于含氧量正常的条件，板在21%氧气，5% CO₂，和74% 氮气中培养(37 ℃)12到14天，而低氧条件下的培养(37℃)在1% 氧气，5% CO₂，和94%氮气的低氧培养室中进行。每个条件下的集落数量在加入50% Alamar Blue，进行荧光检测后评估。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	p-Met / Met / p-Akt / Akt p-MDM2 / p53 / PUMA pROS1 / tROS1 / pSHP2 / pERK / ERK		29854314
	Growth inhibition assay	Cell viability		29854314

体内研究(In Vivo)
体内研究活性	XL880(100 mg/kg，单一剂量，口服强喂)很大程度上抑制B16F10肿瘤Met的磷酸化和配体(比如，HGFor VEGF)诱导的肝脏中Met和肺中Flk-1/KDR受体磷酸化，两者都能持续24小时。XL880 (30-100 mg/kg，每天一次，口服强喂)处理导致肿瘤负荷减少。30和100 mg/kg XL880处理后，肺表面肿瘤负荷分别减少50%和58%。XL880处理负荷B16F10实体瘤的小鼠也会导致剂量依赖性肿瘤生长抑制，30和100 mg/kg分别导致64%和87%的抑制。对于这两项研究，XL880给药具有良好的耐受性，并且没有显著的体重损失。^[1] XL880通过Met可以进一步以HGF的反常信号为作用靶点，同时靶向作用于几个参与肿瘤血管生成的受体酪氨酸激酶。XL880给药2到4小时后，引起人异种移植物中肿瘤出血坏死，96小时(给药5天后)观察到最大肿瘤坏死，导致完全的肿瘤消退。^[3]
动物实验	Animal Models	B16F10 肿瘤细胞(2×10 ⁵)通过胃部静脉注射植入5到8周大的无胸腺裸鼠(NCr 或 BALB/c)
	Dosages	100 mg/kg
	Administration	口服强饲

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00920192	Completed	Carcinoma Hepatocellular	GlaxoSmithKline	August 12 2009	Phase 1
NCT00742261	Completed	Solid Tumours	GlaxoSmithKline	August 11 2008	Phase 1
NCT00725764	Completed	Neoplasms Head and Neck	GlaxoSmithKline	August 27 2007	Phase 2
NCT00725712	Completed	Neoplasms Gastrointestinal Tract	GlaxoSmithKline	March 31 2007	Phase 2
NCT00743067	Completed	Solid Tumours	GlaxoSmithKline	August 9 2006	Phase 1

参考文献
[1] Qian F, et al. Cancer Res, 2009, 69(20), 8009-8016. [2] Kataoka Y, et al. Invest New Drugs, 2011. [3] Eder JP, et al. Clin Cancer Res, 2010, 16(13), 3507-3516.

参考文献

化学信息&溶解度

分子量	632.65	分子式	C₃₄H₃₄F₂N₄O₆
CAS号	849217-64-7	SDF	Download Foretinib SDF
Smiles	COC1=CC2=C(C=CN=C2C=C1OCCCN3CCOCC3)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (158.06 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
批次：

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

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):