PF 477736

Cat. No. 4277

PF 477736 C22H25N7O2 [952021-60-2]

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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 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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

External Portal Information

Chemicalprobes.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.

Technical Data

M.Wt:
419.48
Formula:
C22H25N7O2
Solubility:
Soluble to 75 mM in DMSO
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
952021-60-2

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PF 477736 include:

Meng et al (2015) Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition. J Exp Med 15 422. PMID: 25994202.

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Keywords: PF 477736, supplier, pfizer, PF477736, checkpoint, kinases, chk1, selective, inhibitors, inhibits, dna, damage, cell, cycle, arrest, abrogates, PF0044736, Tocris Bioscience, Checkpoint Kinase Inhibitor products

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