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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
DNA damage detection and repair pathways - recent advances with inhibitors of checkpoint kinases in cancer therapy.
Ashwell and Zabludoff
Clin.Cancer Res., 2008;14:4032
Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1.
Blasina et al.
Mol.Cancer Ther., 2008;7:2394
PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts.
Zhang et al.
Clin.Cancer Res., 2009;15:4630
Citation for PF 477736
The citations listed below are publications that use Tocris products. Selected citations for PF 477736 include:
1 Citation: Showing 1 - 1
Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition.
Authors: Meng Et al.
J Exp Med 2015;15:422
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