CYC-116

CYC-116 is a potent Aurora kinase inhibitor exhibiting Ki values of 8.0 and 9.2 nM for Aurora kinases A and B, respectively. It is significantly less potent against a panel of cyclin-dependent kinases and other related kinases, with the exception of Flt-3 (Ki = 44 nM). CYC-116 exhibits broad-spectrum antiproliferative activity against a panel of human cancer cell lines with a mean IC50 value of 0.54 µM (range = 0.09 - 1.6 µM). It is orally bioavailable and inhibits the growth of human tumor xenografts in mice.Formal Name: 4-(2-amino-4-methyl-5-thiazolyl)-N-[4-(4-morpholinyl)phenyl]-2-pyrimidinamine. CAS Number: 693228-63-6. Molecular Formula: C18H20N6OS. Formula Weight: 368.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1.25 mg/ml, DMSO: 10 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 295, 337 nm. SMILES: CC(N=C(N)S1)=C1C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2. InChi Code: InChI=1S/C18H20N6OS/c1-12-16(26-17(19)21-12)15-6-7-20-18(23-15)22-13-2-4-14(5-3-13)24-8-10-25-11-9-24/h2-7H,8-11H2,1H3,(H2,19,21)(H,20,22,23). InChi Key: GPSZYOIFQZPWEJ-UHFFFAOYSA-N.