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PF-00477736

CAS No. 952021-60-2

PF-00477736( PF00477736 | PF-477736 )

Catalog No. M16807 CAS No. 952021-60-2

PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    PF-00477736
  • Note
    Research use only, not for human use.
  • Brief Description
    PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM).
  • Description
    PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM); displays <100-fold selectivity over VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret, and Yes in a panel of >100 protein kinases; abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin; enhances the antitumor activity of gemcitabine in a dose-dependent manner in xenografts.Solid Tumors Phase 1 Discontinued.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    PF00477736 | PF-477736
  • Pathway
    Angiogenesis
  • Target
    Chk
  • Recptor
    c-Fms|Chk1|Chk2|VEGFR2|Yes
  • Research Area
    Cancer
  • Indication
    Solid Tumors

Chemical Information

  • CAS Number
    952021-60-2
  • Formula Weight
    419.489
  • Molecular Formula
    C22H25N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 31.5 mg/mL (75 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )
  • SMILES
    CN1C=C(C=N1)C2=C3C=NNC(=O)C4=C3C(=CC(=C4)NC(=O)C(C5CCCCC5)N)N2
  • Chemical Name
    (R)-2-amino-2-cyclohexyl-N-(5-(1-methyl-1H-pyrazol-4-yl)-1-oxo-2,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Blasina A, et al. Mol Cancer Ther. 2008 Aug;7(8):2394-404. 2. Zhang C, et al. Clin Cancer Res. 2009 Jul 15;15(14):4630-40.
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