ML-281

ML-281 is an inhibitor of the serine/threonine kinase STK33 (IC50 = 14 nM for purified, recombinant STK33), a kinase whose downregulation is toxic to KRAS-dependent cancer cell lines. It has 700- and 550-fold selectivity for STK33 over PKA and Aurora B kinase, respectively. It is also selective over 81 other kinases in a panel at a concentration of 1 µM, but does inhibit the activity of Fms-like tyrosine kinase (FLT3) and vascular endothelial growth factor receptor 2 (VEGFR2/KDR) by greater than 25%. ML-281 does not decrease viability of KRAS-dependent or KRAS-independent cell lines.Formal Name: N-[2-(3,4-dihydro-3-oxo-2-quinoxalinyl)-4-(1-methylethyl)phenyl]-2-thiophenecarboxamide. CAS Number: 1404437-62-2. Molecular Formula: C22H19N3O2S. Formula Weight: 389.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 20 mg/ml. lambdamax: 284 nm. SMILES: O=C1NC2=CC=CC=C2N=C1C3=C(C=CC(C(C)C)=C3)NC(C4=CC=CS4)=O. InChi Code: InChI=1S/C22H19N3O2S/c1-13(2)14-9-10-16(24-21(26)19-8-5-11-28-19)15(12-14)20-22(27)25-18-7-4-3-6-17(18)23-20/h3-13H,1-2H3,(H,24,26)(H,25,27). InChi Key: HWOYIOLMBQSTQS-UHFFFAOYSA-N.