CHF 78.00
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Product Details
Synonyms PF0477736
Product Type Chemical
Formula C22H25N7O2
MW 419.5
CAS 952021-60-2
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: Chk1 | Kinase Group: CAMK | Substrate: Serine-Threonine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF

Antagonizing the Chk1-mediated cell cycle checkpoints has emerged as an attractive target for anticancer therapy. If Chk1 activity is blocked, DNA-damaged or spindle-disrupted cells would exit cell cycle arrest before full repair and subsequently undergo mitotic catastrophe or cell death. Chk1 inhibitors consequently increase the therapeutic index of DNA-damaging or antimitotic agents as well. PF-0477736 is a selective, potent ATP-competitive Chk1 inhibitor, derived from PF-0394691, inhibits Chk1 (Ki, 0.49nM) and Chk2 (Ki, 47nM) in vitro. In tests, PF-0477736 was identified as a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49nM. PF-0477736 abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin. In xenografts, PF-0477736 enhanced the antitumor activity of gemcitabine in a dose-dependent manner. PF-0477736 combinations were well tolerated with no exacerbation of side effects commonly associated with cytotoxic agents.

Product References
  1. Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1: A. Blasina, et al.; Mol. Cancer Ther. 7, 2394 (2008)
  2. DNA damage detection and repair pathways-recent advances with inhibitors of checkpoint kinases in cancer therapy: S. Ashwell & S. Zabludoff; Clin. Cancer Res. 14, 4032 (2008)
  3. PF-00477736 mediates checkpoint kinase 1 signaling pathway and potentiates docetaxel-induced efficacy in xenografts: C. Zhang, et al.; Clin. Cancer Res. 15, 4630 (2009)
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