BMS777607 Inhibitor CAS No. 1196681-44-3

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KI1195	BMS777607	5 mg	$192
KI1195	BMS777607	10 mg	$336

Chemical Characteristic

Product Name	BMS777607
CAS No.	1196681-44-3
Molecular Weight	512.89
Formula	C₂₅H₁₉ClF₂N₄O₄
Chemical Name	N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
Smiles	c1(=O)c(c(ccn1c1ccc(cc1)F)OCC)C(=O)Nc1cc(c(cc1)Oc1c(c(ncc1)N)Cl)F
Chemical Structure

Biological activities

BMS777607 is a selective and orally efficacious inhibitor of the Met kinase superfamily. The Ki of BMS777607 is 4.6 nM against Met kinase. In contrast, the IC50 of BMS777607 is 3.9 nM against Met kinase. BMS777607 also inhibits Met family member Ron and other three phylogenetically related kinases including Axl, Tyro-3 and Mer. The IC50 of BMS777607 is 1.1, 4.3 and 14 nM against Axl, Tyro-3 and Mer, respectively. BMS777607 prevents Ron with an IC50 of 1.8 nM. The IC50 of BMS777607 is 16 nM against Flt-3. BMS777607 selectively inhibits proliferation in Met-driven tumor cell lines including GTL-16 cells. BMS777607 inhibits proliferation in Met-driven H1993 and U87 cell lines with IC50 of 150 and 160 nM, respectively.^[1] BMS-777607 exhibits inhibitory effect on HGF-induced cell scattering in PC-3 and DU145 cells. BMS-777607 at the dose of 0.5 µM almost completely prevents cell spreading. Doses of 3 and 10 µM BMS-777607 significantly reduce the HGF-induced cell proliferation without apparent cytotoxicity. ^[2] BMS-777607 also potently inhibits phosphorylation of c-Met and downstream pathway. ^[3] Intravenous injections of BMS777607 exhibit a moderate steady-state volume of distribution (V_{ss) in mouse and rat and low systemic clearance (Cl) compared to hepatic blood flow. Orally injection of BMS777607 is well absorbed from solution formulation with favorable half-lives (t_{1/2) and mean residence times (MRT). ^[1] The IC50 of BMS777607 is 20 nM against autophosphorylation of c-Met. BMS777607 impairs xenograft growth.^[1] BMS-777607 at the dose of 25 mg/kg/day significantly decreases the number of KHT lung tumor nodules by 28.3%.^[3]}}

Protocols

In vitro BMS777607 is dissolved in DMSO and stored as aliquots (10 mM) at -20°C.^[2]

References

[1] Schroeder GM, et al. Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. J Med Chem. 2009, 52(5): 1251-1254. [2] Dai Y, et al. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther. 2010, 9(6): 1554-1561. [3] Dai Y, Bae K, et al. Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation. Clin Exp Metastasis. 2012, 29(3): 253-261.

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