R&D Systems Inc. Tocris Bioscience Boston Biochem

PHA 665752

Cat. No. 2693

PHA 665752 C32H34Cl2N4O4S [477575-56-7]

Price and Availability

For PHA 665752 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

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

Biological Activity

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

M.Wt:
641.61
Formula:
C32H34Cl2N4O4S
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
477575-56-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Select another batch:
Safety Data Sheet: View Safety Data Sheet

References

Christensen et al (2003) 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. 63 7345. PMID: 14612533.

Smolen et al (2006) 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 103 2316.

Puri et al (2007) A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res. 67 3529. PMID: 17440059.

Tu et al (2010) Efficacy of c-Met inhibitor for advanced prostate cancer. BMC Cancer 10 556. PMID: 20946682.

If you know of a relevant citation for this product please let us know.

Keywords: PHA 665752, supplier, Potent, selective, cMET, inhibitors, Hepatocyte, Growth, Factors, Receptors, HGFR, Receptor, Tyrosine, Kinases, RTKs, PHA665752, Pfizer

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Guide

Highlights over 350 products for cancer research. Request a copy or view PDF today.

divider line

Kinases Product Listing

Kinases Product Listing

Highlights over 350 products for kinase research. Request a copy or view PDF today.

divider line

Kinase Inhibitor Toolbox

80 Kinase inhibitors
pre-dissolved in DMSO

Kinase Inhibitor Toolbox

Includes many of the latest kinase inhibitors to become commercially available. Covers a wide range of kinase targets including EGFR, MAPK and CDK.

divider line

VEGF Pathway & Anti-Angiogenic Therapy

Written by N. Ferrara & Y. Crawford

Angiogenesis Poster

A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance.

divider line

New Product Guide

NPG

Highlights 150 new products added in the second half of 2014. View PDF today.

divider line

New Products in this Area

AEE 788

Potent EGFR and VEGFR inhibitor

XL 184

Potent VEGFR inhibitor; also inhibits other RTKs

PKI 166 hydrochloride

Potent EGFR-kinase inhibitor

ASP 3026

Potent anaplastic lymphoma kinase (ALK) inhibitor

KYL

EphA4 receptor tyrosine kinase inhibitor; neuroprotective

PD 90780

Inhibits NGF binding to p75NTR

LM11A 31 dihydrochloride

Nonpeptide p75NTR ligand; neuroprotective

EG 00229

Neuropilin 1 (NRP1) receptor antagonist; inhibits VEGFA binding to NRP1

Sign-up for new product e-alerts
divider line

Bio-Techne Events

DPG 2015

94th Meeting of the German Physiological Society

March 5 - 7, 2015

Magdeburg, Germany