849217-64-7

EXEL-2880/XL880/GSK1363089/Foretinib

849217-64-7

编号ABP000883 化学名称EXEL-2880/XL880/GSK1363089/Foretinib 英文名称 EXEL-2880/XL880/GSK1363089/Foretinib 分子式C34H34F2N4O6 分子量632.6538 纯度 98%

化学名称 : EXEL-2880/XL880/GSK1363089/Foretinib

CAS : 849217-64-7

英文名称: EXEL-2880/XL880/GSK1363089/Foretinib

英文同义词: N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide

溶解度:DMSO

储存条件:at -20℃ 2 years

生物活性

A potent and selective inhibitor of tyrosine kinases, targeting VEGFR/c-KIT/PDGFR, blocking angiogenesis; as an oral antineoplastic agent.VEGFR enzyme assays for VEGGR1,VEGFR2, and VEGFR3 were running in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3.
Pazopanib showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFR beta, c-Kit, FGF-R1, and c-fms with IC50’s of 84, 74, 140,and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibited VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ∼8 nM.
 

参考文献

G Sonpavde et al. Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma. Exp. Opin. Invest. Drugs. 2008, 17(2), 253-261. G Sonpavde and TE Hutson. Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr. Oncol. Rep. 2007, 9(2), 115-9. K Podar et al. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma. Proc. Natl. Acad. Sci. USA. 2006, 103(51), 19478-19483

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