Catalog Number: 4277
Alternate Names: 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 Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 75 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. 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
  2. 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
  3. PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts.
    Zhang et al.
    Clin.Cancer Res., 2009;15:4630

The citations listed below are publications that use Tocris products. Selected citations for PF 477736 include:

Showing Results 1 - 1 of 1

  1. Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition.
    Authors: Meng Et al.
    J Exp Med
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details


Contact Information

Molarity Calculator
Calculate the mass, volume or concentration required for a solution

The molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) x Volume (L) x Molecular Weight (g/mol)
An example of a molarity calculation using the molarity calculator:
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?

R&D Systems Guarantee

or select another batch:


Customer Information