产品名称

英文名称：Foretinib (GSK1363089)

同义词

Foretinib、849217-64-7、GSK1363089、XL880、EXEL-2880、Foretinib (GSK1363089)、GSK089、XL-880、GSK 1363089、XL 880、EXEL 2880、GSK-1363089、Foretinib(XL880)、GSK-089、GSK1363089G、81FH7VK1C4、GSK-1363089G、937176-80-2、N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-

产品性质

CAS编号：849217-64-7

分子式：C34H34F2N4O6

分子量：632.65

PubChem编号：42642645

英文别名：Foretinib|849217-64-7|GSK1363089|XL880|EXEL-2880|Foretinib (GSK1363089)|GSK089|XL-880|GSK 1363089|XL 880|EXEL 2880|GSK-1363089|Foretinib(XL880)|GSK-089|GSK1363089G|81FH7VK1C4|GSK-1363089G|937176-80-2|N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-

规格或纯度：≥98%

英文名称：Foretinib (GSK1363089)

生化机理：MET，VEGFR2，Ron和AXL的有效抑制剂（IC50值分别为0.4、0.9、3和11 nM）。还有效抑制Tie-2，Flt-1，Flt-3，Flt-4，KIT，PDGFRα和PDGFRβ。在体外抑制B16F10黑色素瘤细胞的迁移和侵袭。抑制小鼠中的B16F10肿瘤生长和转移。口服。

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：5mg、100mg卖完停产，不再备货

产品介绍：Foretinib (GSK1363089)是一种ATP竞争性的HGFR和VEGFR抑制剂，作用于Met和KDR作用最强，IC50分别为0.4 nM和0.9 nM，对Ron， Flt-1/3/4， Kit， PDGFRα/β和Tie-2作用效果稍弱，对FGFR1和EGFR几乎没有抑制活性。An ATP-competitive inhibitor of tyrosine kinases including Flt-1, Flt-4, Met, and Ron.Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFRAn ATP-competitive inhibitor of tyrosine kinases including Flt-1, Flt-4, Met, and Ron.

ALogP：5.5

IUPAC Name：1-N'-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

INCHI：InChI=1S/C34H34F2N4O6/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42)

InChi Key：CXQHYVUVSFXTMY-UHFFFAOYSA-N

Canonical 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

Isomeric 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

PubChem CID：42642645

CAS Registry No.：849217-64-7

Wikipedia：Foretinib

DiscoveRx TREEspot：EXEL-2880/GSK-1363089|

ChEMBL Ligand：CHEMBL1230609

RCSB PDB Ligand：88Z

溶解性：溶于DMSO, 最高浓度 (mg/mL) 63.26, 最高浓度(mM) 100；溶于ethanol, 最高浓度 (mg/mL) 63.26, 最高浓度(mM) 100

象形图：

信号词：Warning

危险声明：H373 Causes damage to organs through prolonged or repeated exposureH302 Harmful if swallowed

预防措施声明：P501,P264,P260,P270,P330,P301+P317,P319

产品包装