CHIR124

Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. CHIR124 is a cell-permeable, quinolone-based inhibitor of Chk1 (IC50 = 0.3 nM in vitro). It demonstrates high selectivity for Chk1 by displaying inhibitory values 2,000-fold higher against Chk2 (IC50 = 0.7 µM). In synergy with topoisomerase I poisons or ionizing radiation, CHIR124 can inhibit the growth of p53-mutant solid tumor cells both in vitro and in a xenograft model, potentiating tumor apoptosis.Formal Name: 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro-2(1H)-quinolinone. CAS Number: 405168-58-3. Molecular Formula: C23H22ClN5O. Formula Weight: 419.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 10 mg/ml. lambdamax: 241, 288, 375 nm. SMILES: O=C(C(C1=NC2=C(C=CC=C2)N1)=C3N[C@@H]4CN5CCC4CC5)NC6=C3C=C(Cl)C=C6. InChi Code: InChI=1S/C23H22ClN5O/c24-14-5-6-16-15(11-14)21(25-19-12-29-9-7-13(19)8-10-29)20(23(30)28-16)22-26-17-3-1-2-4-18(17)27-22/h1-6,11,13,19H,7-10,12H2,(H,26,27)(H2,25,28,30)/t19-/m1/s1. InChi Key: MOVBBVMDHIRCTG-LJQANCHMSA-N.