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

Description:	Potent and selective MET inhibitor
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% (HPLC)
Molecular Weight:	641.61

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data for PHA 665752

M. Wt	641.61
Formula	C₃₂H₃₄Cl₂N₄O₄S
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	477575-56-7
PubChem ID	10461815
InChi Key	OYONTEXKYJZFHA-SSHUPFPWSA-N
Smiles	ClC1=C(CS(C2=CC(/C(C(N4)=O)=C/C3=C(C)C(C(N5CCC[C@@H]5CN6CCCC6)=O)=C(C)N3)=C4C=C2)(=O)=O)C(Cl)=CC=C1

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

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	64.16	100

Preparing Stock Solutions for PHA 665752

The following data is based on the product molecular weight 641.61.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.56 mL	7.79 mL	15.59 mL
5 mM	0.31 mL	1.56 mL	3.12 mL
10 mM	0.16 mL	0.78 mL	1.56 mL
50 mM	0.03 mL	0.16 mL	0.31 mL

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References for PHA 665752

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

Smolen 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
Puri A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res. 2007 PMID: 17440059
Tu Efficacy of c-Met inhibitor for advanced prostate cancer. BMC Cancer 2010 PMID: 20946682
Christensen 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 PMID: 14612533