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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 |