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PF-0477736

Product Details | |
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Synonyms | PF0477736 |
Product Type | Chemical |
Properties | |
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. |
InChi Key | NDEXUOWTGYUVGA-LJQANCHMSA-N |
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. |
Documents | |
MSDS |
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Product Specification Sheet | |
Datasheet |
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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.
- 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)
- 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)
- 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)