Overview

  • Product name

    PHA-665752, c-Met inhibitor
  • Description

    Potent, selective, ATP-competitive c-Met inhibitor
  • Alternative names

    • PHA 665752
    • PHA665752
  • Biological description

    Potent, selective, ATP-competitive c-Met inhibitor (Ki = 4 nM; IC50 = 9 nM). Exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.

  • Purity

    > 99%
  • CAS Number

    477575-56-7
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (R,Z)-5-(2,6-Dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one
  • Molecular weight

    641.61
  • Molecular formula

    C32H34Cl2N4O4S
  • PubChem identifier

    10461815
  • Storage instructions

    Store at -20°C. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CC1=C(NC(=C1C(=O)N2CCC[C@@H]2CN3CCCC3)C)/C=C\4/C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O
  • Source

    Synthetic

References

This product has been referenced in:

  • Yang Y  et al. A selective small molecule inhibitor of c-Met, PHA-665752, reverses lung premalignancy induced by mutant K-ras. Mol Cancer Ther 7:952-60 (2008). Read more (PubMed: 18413809) »
  • Puri N  et al. A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res 67:3529-34 (2007). Read more (PubMed: 17440059) »
  • Ma PC  et al. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res 11:2312-9 (2005). Read more (PubMed: 15788682) »
  • Christensen JG  et al. 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 63:7345-55 (2003). Read more (PubMed: 14612533) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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