Cat. No. 4277
Alternative Name: PF-0044736
Chemical Name: (R)-α-Amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide
Biological ActivitySelective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage. Enhances docetaxel (Cat. No. 4056) efficacy in tumor cells and xenografts.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Ashwell and Zabludoff (2008) DNA damage detection and repair pathways - recent advances with inhibitors of checkpoint kinases in cancer therapy. Clin.Cancer Res. 14 4032. PMID: 18593978.
Blasina et al (2008) Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol.Cancer Ther. 7 2394. PMID: 18723486.
Zhang et al (2009) PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts. Clin.Cancer Res. 15 4630. PMID: 19584159.
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Keywords: PF 477736, supplier, pfizer, PF477736, checkpoint, kinases, chk1, selective, inhibitors, inhibits, dna, damage, cell, cycle, arrest, abrogates, PF0044736
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