PF 477736
Tocris Bioscience, part of Bio-Techne | Catalog # 4277
Selective Chk1 inhibitor
Discontinued Product
4277 has been discontinued.
View all Checkpoint Kinase Inhibitors products.
Key Product Details
Description
Selective Chk1 inhibitor
Alternative Names
PF-0044736
Product Description
PF 477736 is a 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.Product Specifications
Molecular Weight
419.48
Formula
C22H25N7O2
Storage
Store at +4°C
Purity
≥99% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for PF 477736
For research use only
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