Chemical Name : EXEL-2880/XL880/GSK1363089/Foretinib
CAS : 849217-64-7
Storage:at -20℃ 2 years
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.
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