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Catalog No.
C-Met inhibitor,potent and ATP-competitive
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SizePriceStock Qty
10mM (in 1mL DMSO)
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Evaluation Sample
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PHA-665752 is a potent, ATP-competitive and specific c-Met receptor tyrosine kinase inhibitor with K(i) value of 4 nM and IC50 value of 9nM. PHA-665752 shows more than 50-fold selectivity for c-Met versus other serine-threonine and tyrosine kinases [1].

PHA-665752 has been demonstrated to inhibit hepatocyte growth factor (HGF) and c-Met-mediated cell proliferation, motility, invasion and morphology of pancreatic carcinoma cells BxPC-3, gastric carcinoma cells GTL-16 and lung cancer cells NCI-H441. Additionally, PHA-665752 inhibits the c-MET downstream mediators phosphorylation induced by HGF [1].

In vivo, PHA-665752 inhibits c-Met phosphorylation as well as tumor growth in both S114 and GTL-16 implanted xenograft athymic mice [1].

[1] Christensen JG1, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ,Cherrington JM, Mendel DB. 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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.477575-56-7
Solubility≥32.1mg/mL in DMSO
Chemical Name(3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one
SDFDownload SDF
Canonical SMILESCC1=C(NC(=C1C(=O)N2CCCC2CN3CCCC3)C)C=C4C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description PHA-665752 is a potent, selective and ATP-competitive inhibitor of c-Met with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.
Targets c-Met          
IC50 9 nM          

Quality Control

Quality Control & MSDS

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Chemical structure


Related Biological Data


Related Biological Data


Related Biological Data


Research Update

1. Celastrol exerts synergistic effects with PHA-665752 and inhibits tumor growth of c-Met-deficient hepatocellular carcinoma in vivo. Mol Biol Rep. 2013 Jul;40(7):4203-9. doi: 10.1007/s11033-013-2501-y. Epub 2013 May 7.
PHA665752 is a c-Met inhibitor that exhibits anti-tumor activity only in c-Met-positive tumor cells. The combination of PHA6657552 and Celastrol is a potential therapy of c-Met-deficient tumors for their demonstrated antitumor effects in c-Met-deficient hepatocellular carcinoma cells and xenografts.
2. A selective small molecule inhibitor of c-Met, PHA-665752, reverses lung premalignancy induced by mutant K-ras. Mol Cancer Ther. 2008 Apr;7(4):952-60. doi: 10.1158/1535-7163.MCT-07-2045.
PHA-665752, a c-Met inhibitor, inhibited lung tumorigenesis in Kras(LA1) mice and induced apoptosis in LKR-13 cells and MECs, where apoptosis in MECs was induced by c-Met inhibition.
3. Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A. 2006 Feb 14;103(7):2316-21. Epub 2006 Feb 6.
Gastric cancer cells with high levels of MET are extraordinarily susceptible to PHA-665752, which induces massive apoptosis.