PZ0186

PF-477736

≥98% (HPLC)

• Synonym(s): (2R)-2-Amino-2-cyclohexyl-N-[2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl]-acetamide, PF-00477736
• Empirical Formula (Hill Notation): C₂₂H₂₅N₇O₂
• CAS Number: 952021-60-2
• Molecular Weight: 419.48
• MDL number: MFCD16038847
• UNSPSC Code: 12352200
• PubChem Substance ID: 329823760
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• form: powder
• color: yellow
• solubility: DMSO: ≥20 mg/mL
• storage temp.: 2-8°C
• SMILES string: Cn1cc(cn1)-c2[nH]c3cc(NC(=O)[C@H](N)C4CCCCC4)cc5C(=O)NN=Cc2c35
• InChI: 1S/C22H25N7O2/c1-29-11-13(9-25-29)20-16-10-24-28-21(30)15-7-14(8-17(27-20)18(15)16)26-22(31)19(23)12-5-3-2-4-6-12/h7-12,19,27H,2-6,23H2,1H3,(H,26,31)(H,28,30)/t19-/m1/s1
• InChI key: NDEXUOWTGYUVGA-LJQANCHMSA-N

Description

Application

PF-477736 has been used as a checkpoint protein 1 (CHK1) inhibitor to study the effect of CHK1 in cell cycle regulation in primary breast and lung primary epithelial cells.

Biochem/physiol Actions

PF-00477736 is a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49 nM. The compound abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin.

PF-477736 may be effectively used to resensitize platinum resistant ovarian cancer cells. PF-477736 alone or in combination with other chemotherapeutic agents may be used to treat triple-negative breast cancer.

Other Notes

PF-477736 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PF-477736 probe summary on the Chemical Probes Portal website.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable