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.

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

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.

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

Keywords: PF 477736, supplier, pfizer, PF477736, checkpoint, kinases, chk1, selective, inhibitors, inhibits, dna, damage, cell, cycle, arrest, abrogates, PF0044736

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