PHA 665752

• Supplier: Tocris Bioscience
• Catalog: 3134
• Prices: $289.00, $1,185.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 477575-56-7
• Chemical Name: (2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine
• Formula: C32H34Cl2N4O4S
• Molecular Weight: 641.61
• Purity: >98 %
• Description: Potent, selective and ATP-competitive inhibitor of MET kinase (IC 50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKB α , p38 α , MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.

Product References

A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent - A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent

Christensen JG, 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. Cancer Res. 2003 Nov 1;63(21):7345-55.

A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity - A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity

Puri N, Khramtsov A, Ahmed S, Nallasura V, Hetzel JT, Jagadeeswaran R, Karczmar G, Salgia R. Cancer Res. 2007 Apr 15;67(8):3529-34.

Efficacy of c-Met inhibitor for advanced prostate cancer. - Efficacy of c-Met inhibitor for advanced prostate cancer.

Tu WH, Zhu C, Clark C, Christensen JG, Sun Z. BMC Cancer. 2010 Oct 14;10:556.