PF-477736

Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2. When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.Formal Name: (alphaR)-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. Molecular Formula: C22H25N7O2. Formula Weight: 419.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml. lambdamax: 265, 330 nm. SMILES: O=C([C@H](N)C1CCCCC1)NC2=CC3=C4C(NC(C5=CN(C)N=C5)=C4C=NNC3=O)=C2. InChi Code: 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.