PHA 665752

Name: PHA 665752
Brand: Tocris Bioscience
SKU: 2693

Tocris Bioscience, part of Bio-Techne | Catalog # 2693

Citations (108)

COA / SDS

Potent and selective MET inhibitor

Key Product Details

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
Purity:	≥98%
Molecular Weight:	641.61 kDa

View Full Technical Details for PHA 665752

Technical Data
Citations

Biological Activity for PHA 665752

PHA 665752 is a potent, selective and ATP-competitive inhibitor of MET kinase (IC₅₀ 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, PKBα, p38α, MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.

Technical Data for PHA 665752

M. Wt	641.61 kDa
Formula	C₃₂H₃₄Cl₂N₄O₄S
Storage	Store at +4°C
Purity	≥98%
CAS Number	477575-56-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PHA 665752

Solubility

Soluble Soluble to 100 mM in DMSO

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References for PHA 665752

References are publications that support the biological activity of the product.

Saito S, Morishima K, Ui T, Hoshino H, Matsubara D, Ishikawa S, Aburatani H, Fukayama M, Hosoya Y, Sata N, Lefor A, Yasuda Y, Niki T The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma. BMC Cancer, 2015;15(0):82. 2015 PMID: 25884729
Yoshimoto A, Bernardazzi C, Carneiro A, Elia C, Martinusso C, Ventura G, Castelo-Branco M, de Souza H Hedgehog pathway signaling regulates human colon carcinoma HT-29 epithelial cell line apoptosis and cytokine secretion. PLoS ONE, 2012;7(9):e45332. 2012 PMID: 23028941
Wiener Z, Band A, Kallio P, Hogstrom J, Hyvonen V, Kaijalainen S, Ritvos O, Haglund C, Kruuna O, Robine S, Louvard D, Ben-Neriah Y, Alitalo K Oncogenic mutations in intestinal adenomas regulate Bim-mediated apoptosis induced by TGF-beta. Proc Natl Acad Sci U S A, 2014;111(21):E2229-36. 2014 PMID: 24825889
Basilico C, Pennacchietti S, Vigna E, Chiriaco C, Arena S, Bardelli A, Valdembri D, Serini G, Michieli P Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET. Clin Cancer Res, 2013;19(9):2381-92. 2013 PMID: 23532890
Accornero, Paolo, Miretti, Silvia, Bersani, Francesc, Quaglino, Elena, Martignani, Eugenio, Baratta, Mario Met receptor acts uniquely for survival and morphogenesis of EGFR-dependent normal mammary epithelial and cancer cells. PLoS ONE, 2012;7(9):e44982. 2012 PMID: 23028720
Lee Y, Park H, Woo S, Park E, Kang J RhoA/phosphatidylinositol 3-kinase/protein kinase B/mitogen-activated protein kinase signaling after growth arrest-specific protein 6/mer receptor tyrosine kinase engagement promotes epithelial cell growth and wound repair via upregulation of hepatocyte growth factor in macrophages. J Pharmacol Exp Ther, 2014;350(3):563-77. 2014 PMID: 24939420
E Paldy, M Simonetti, T Worzfeld, KK Bali, L Vicuña, S Offermanns, R Kuner Semaphorin 4C Plexin-B2 signaling in peripheral sensory neurons is pronociceptive in a model of inflammatory pain Nat Commun, 2017;8(1):176. 2017 PMID: 28765520
Christensen et al. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumour activity in vivo. Cancer Res., 2003;63:7345 PMID: 14612533
Puri et al. A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res., 2007;67:3529 PMID: 17440059
Tu et al. Efficacy of c-Met inhibitor for advanced prostate cancer. BMC Cancer, 2010;10:556 PMID: 20946682
Smolen et al. Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc.Natl.Acad.Sci.USA, 2006;103:2316