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 ActivityPF 477736 is a selective 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.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 477736 is reviewed on the chemical probes website.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
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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