CCT245737

CCT245737 is a potent inhibitor of checkpoint kinase 1 (Chk1, IC50 = 1.3 nM). It is selective for Chk1 over Chk2 (IC50 = 2,440 nM). CCT245737 inhibits G2 checkpoint arrest induced by etoposide (Cay-12092) in HT-29 colon cancer cells (IC50 = 30 nM). In vivo, CCT245737 (300 mg/kg) inhibits Chk1 autophosphorylation induced by gemcitabine (Cay-11690) in an SW620 colon cancer mouse xenograft model. It reduces tumor volume when administered alone or in combination with gemcitabine in an HT-29 mouse xenograft model. CCT245737 (150 mg/kg) reduces inguinal, brachial/axillary, and mesenteric lymph node weights in the Eµ-Myc driven transgenic mouse transplant model of lymph gland-infiltrating B cell lymphoma.Formal Name: 5-[[4-[[(2R)-2-morpholinylmethyl]amino]-5-(trifluoromethyl)-2-pyridinyl]amino]-2-pyrazinecarbonitrile. CAS Number: 1489389-18-5. Molecular Formula: C16H16F3N7O. Formula Weight: 379.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 224, 293, 339 nm. SMILES: FC(F)(F)C(C=N1)=C(NC[C@@H]2OCCNC2)C=C1NC3=CN=C(C#N)C=N3. InChi Code: InChI=1S/C16H16F3N7O/c17-16(18,19)12-8-25-14(26-15-9-22-10(4-20)5-24-15)3-13(12)23-7-11-6-21-1-2-27-11/h3,5,8-9,11,21H,1-2,6-7H2,(H2,23,24,25,26)/t11-/m1/s1. InChi Key: YBYYWUUUGCNAHQ-LLVKDONJSA-N.