PF 477736

Key Product Details

Product Description

PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (K_i 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.

Product Specifications for PF 477736

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PF 477736

The following data is based on the product molecular weight 419.48.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.75 mM	3.18 mL	15.89 mL	31.79 mL
3.75 mM	0.64 mL	3.18 mL	6.36 mL
7.5 mM	0.32 mL	1.59 mL	3.18 mL
37.5 mM	0.06 mL	0.32 mL	0.64 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 12 publications citing the usage of this product.

• Blasina Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol.Cancer Ther. 2008 PMID: 18723486
• Zhang PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts. Clin.Cancer Res. 2009 PMID: 19584159
• Ashwell and Zabludoff DNA damage detection and repair pathways - recent advances with inhibitors of checkpoint kinases in cancer therapy. Clin.Cancer Res. 2008 PMID: 18593978

Product Documents for PF 477736