Loading... Please wait...

Categories

Our Newsletter


BMS-777607 | Met/Axl/Ron inhibitor

  • BMS-777607.jpg
  • BMS-777607, 400x400px, png
Price:
$129.00
Catalog #:
C2777-5
Quantity:


Product Description

BMS-777607 is an orally available, ATP-competitive Met kinase inhibitor with IC50 of 3.9 nM with additional activity against related kinases such as Axl and Ron at 1.1 nM, and 1.8 nM, respectively [1] BMS-777607 blocks autophosphorylation of c-Met at and IC50 of 20 nM and also blocks downstream activation of Akt and extracellular signal-regulated kinases. [2]

Because of its added ability to suppress HGF-stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 100 nM), BMS-777607 is being considered as a potential for the treatment of advanced prostate cancer. [2]

Additional studies have shown that BMS-777607 suppressed c-Met-associated cellular funcdtions in PC-3 cells expressing constitutively activated c-Met; these findings suggest the possibility that in cancers where hyperactive c-Met is independent of HGF-mediated autocrine stimulation, targeting Met may be more effective than targeting the HGF ligand to impede cancer progression and metastasis. [3]


Technical information:

Chemical Formula:   C25H19ClF2N4O4
CAS #:   1196681-44-3
Molecular Weight:   512.89
Purity:   >98%
Appearance:   White
Chemical Name:   N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
Solubility:   Up to 75 mM in DMSO
Synonyms:   BMS-777607, BMS 777607, BMS777607

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

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 Pubmed ID: 19260711
2. Dai 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, 1554-1561. Pubmed ID: 20515943
3. Dai et al., Constitutively active c-Met kinase in PC-3 cells is autocrine-independent and can be blocked by the Met kinase inhibitor BMS-777607. BMC Cancer 2012, 12, 198-206. Pubmed ID: 22639908

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the BMS-777607 | Met/Axl/Ron inhibitor to your wish list.

You Recently Viewed...