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PHA-665752

Catalog No.
A2307
C-Met inhibitor,potent and ATP-competitive
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$90.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$80.00
In stock
50mg
$330.00
In stock
100mg
$570.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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].

References:
[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
M.Wt641.61
Cas No.477575-56-7
FormulaC32H34Cl2N4O4S
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 sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C 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

PHA-665752

Related Biological Data

PHA-665752

Related Biological Data

PHA-665752

Related Biological Data

PHA-665752