PF 477736

Name: PF 477736
Brand: Tocris Bioscience
SKU: 4277

Tocris Bioscience, part of Bio-Techne | Catalog # 4277

Citations (8)

COA / SDS

Selective Chk1 inhibitor

Key Product Details

Description:	Selective Chk1 inhibitor
Alternative 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
Purity:	≥99% (HPLC)
Molecular Weight:	419.48

View Full Technical Details for PF 477736

Technical Data
Citations

Biological Activity for PF 477736

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.

Compound Libraries for PF 477736

PF 477736 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

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 for PF 477736

M. Wt	419.48
Formula	C₂₂H₂₅N₇O₂
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	952021-60-2
PubChem ID	16750408
InChi Key	YFNWWNRZJGMDBR-LJQANCHMSA-N
Smiles	O=C([C@H](N)C4CCCCC4)NC1=CC3=C(C(C=NNC3=O)=C(C5=CN(C)N=C5)N2)C2=C1

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.

Solubility for PF 477736

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	31.46	75

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for PF 477736

References are publications that support the biological activity of the 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