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BMS-777607C-Met inhibitor, potent and selective

BMS-777607

Catalog No. A5703
Size Price Stock Qty
10mM (in 1mL DMSO) $85.00 In stock
Evaluation Sample $28.00 In stock
5mg $80.00 In stock
25mg $250.00 In stock
100mg $680.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BMS-777607

Related Biological Data

BMS-777607

Related Biological Data

BMS-777607

Biological Activity

Description BMS-777607 is an inhibitor of Met-related for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
Targets c-Met Axl Ron Tyro3    
IC50 3.9 nM 1.1 nM 1.8 nM 4.3 nM    

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Chemical Properties

Cas No. 1025720-94-8 SDF Download SDF
Chemical Name N-[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide
Canonical SMILES CCOC1=C(C(=O)N(C=C1)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F
Formula C25H19ClF2N4O4 M.Wt 512.89
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

BMS 777607 is a novel, selective and orally available ATP-competitive MET kinase inhibitor that primarily targets several MET family members, including RON, MET, Tyro-3 and AxI, with half maximal inhibitory concentration IC50 of 1.8 nmol/L, 3.9 nmol/L, 4.3 nmol/L and 1.1 nmol/L respectively. Moreover, at higher concentrations, BMS 777607 has been found to inhibit other protein tyrosine kinases, including Mer, Flt-3, Aurora B, Lck and VEGFR2 with IC50 of 14 nmol/L, 16 nmol/L, 78 nmol/L, 120 nmol/L and 180 nmol/L respectively. In previous studies, BMS 777607 potently inhibited the auto-phosphorylation of c-MET (IC50: 20 nmol/L) leading to impaired xenograft growth.

References:
[1]Dai Y, Siemann DW. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther. 2010 Jun;9(6):1554-61. doi: 10.1158/1535-7163.MCT-10-0359. Epub 2010 Jun 1.
[2]Sharma S, Zeng JY, Zhuang CM, Zhou YQ, Yao HP, Hu X, Zhang R, Wang MH.

Small-molecule inhibitor BMS-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents. Mol Cancer Ther. 2013 May;12(5):725-36. doi: 10.1158/1535-7163.MCT-12-1079. Epub 2013 Mar 6.