OTS514

OTS514 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK, IC50 = 2.6 nM), a serine-threonine kinase often overexpressed and transactivated in several types of cancer. OTS514 (10 nM) selectively inhibits growth of patient-derived acute myeloid leukemia (AML) cells over normal CD34+ cells. It shows similar growth inhibitory effects in multiple small cell lung, kidney, and ovarian cancer cell lines (IC50s = 0.4-42.6 nM). In vivo, OTS514 (25 and 50 mg/kg) increases survival in a peritoneal mouse dissemination model of ovarian cancer. It also dose-dependently inhibits tumor growth in an A549 mouse xenograft model when administered at doses of 1, 2.5, and 5 mg/kg.Formal Name: 9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one. CAS Number: 1338540-63-8. Molecular Formula: C21H20N2O2S. Formula Weight: 364.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml. lambdamax: 219, 233, 297, 351 nm. SMILES: CC1=C2C(C(C=CS3)=C3C(N2)=O)=C(C4=CC=C([C@@H](C)CN)C=C4)C(O)=C1. InChi Code: InChI=1S/C21H20N2O2S/c1-11-9-16(24)17(14-5-3-13(4-6-14)12(2)10-22)18-15-7-8-26-20(15)21(25)23-19(11)18/h3-9,12,24H,10,22H2,1-2H3,(H,23,25)/t12-/m0/s1. InChi Key: OETLNMOJNONWOY-LBPRGKRZSA-N.