PHA-665752

PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM) . PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity[1][2].

Product Specifications

CAS Number

[477575-56-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; c-Met/HGFR

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PHA-665752.html

Concentration

10mM

Purity

99.85

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(C1=C(NC(/C=C2C(NC3=C\2C=C(C=C3)S(=O)(CC4=C(C=CC=C4Cl)Cl)=O)=O)=C1C)C)N5[C@H](CCC5)CN6CCCC6

Molecular Formula

C32H34Cl2N4O4S

Molecular Weight

641.61

Precautions

H302, H315, H319, H335

References & Citations

[1]Christensen JG, et al. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003 Nov 1;63 (21) :7345-55.|[2]Ma PC. et al. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res. 2005 Mar 15;11 (6) :2312-9.