Loading... Please wait...

Our Newsletter

PHA-665752 | cMET/RON inhibitor

  • PHA-665752.jpg
  • PHA-665752, 400x400px, png
Catalog #:

Product Description

PHA-665752 is an oxindole-based, ATP-competitive c-Met and Ron inhibitor with IC50 potencies of 9 nM, and 68 nM, respectively. [1] It is >50-fold selective compared to a broad panel of both tyrosine and serine-threonine kinases. In cellular studies, PHA-665752 inhibits HGF-stimulated and constitutive c-Met phosphorylation as well as downstream signal transduction mediators such as Gab-1, Akt, phospholipase C gamma, and focal adhesion kinase. Inhibition of c-Met phosphorylation is dose-dependent and correlates well with tumor growth inhibition.

PHA-665752 induced apoptosis and cell cycle arrest in BaF3.TPR-MET cells at an IC50 of 60 nM. [2] Additionally, PHA-665752 has been suggested to inhibit lung tumorigenesis in mutant K-Ras mice and may be a formidable treatment for NSCLC. [3]

Technical information:

Chemical Formula:   C32H34Cl2N4O4S
CAS #:   477575-56-7
Molecular Weight:   641.61
Purity:   >98%
Appearance:   Yellow
Chemical Name:   (R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one
Solubility:   Up to 100 mM in DMSO
Synonyms:   PHA-665752, PHA 665752, PHA665752

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.


1. Christensen 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, 63, 7345-7355. Pubmed ID: 14612533
2. Ma et al., A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin. Cancer Res. 2005, 11, 2312-2139 Pubmed ID: 15788682
3. Yang et al., A selective small molecule inhibitor of c-Met, PHA-665752, reverses lung premalignancy induced by mutant K-ras. Mol. Cancer Ther. 2008, 7, 952-960. Pubmed ID: 18413809

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 PHA-665752 | cMET/RON inhibitor to your wish list.

You Recently Viewed...