PHA-665752

• Description:

  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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  477575-56-7