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Submit ReviewPF 477736
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)
Biological Activity for PF 477736
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 for PF 477736
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.
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.
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 Data for PF 477736
| 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 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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Product Datasheets for PF 477736
References for PF 477736
References are publications that support the biological activity of the product.
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 reference for PF 477736, please let us know.
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Keywords: PF 477736, PF 477736 supplier, pfizer, PF477736, checkpoint, kinases, chk1, selective, inhibitors, inhibits, dna, damage, cell, cycle, arrest, abrogates, PF0044736, PF-0044736, Checkpoint, Kinases, Control, 4277, Tocris Bioscience
3 Citations for PF 477736
Citations are publications that use Tocris products. Selected citations for PF 477736 include:
Damarys et al (2020) Histone variant H3.3 residue S31 is essential for Xenopus gastrulation regardless of the deposition pathway. Nat Commun 11 1256 PMID: 32152320
Meng et al (2015) Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition. J Exp Med 15 422 PMID: 25994202
Daniel P et al (2021) Replication stress promotes cell elimination by extrusion. Nature 593 591-596 PMID: 33953402
Do you know of a great paper that uses PF 477736 from Tocris? Please let us know.
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Literature in this Area
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.