LFM-A13

LFM-A13 is an inhibitor of Bruton's tyrosine kinase (BTK, IC50 = 2.5 µM). It is selective for BTK over JAK1, JAK3, IRK, EGFR, and HCK (IC50s = >278 µM for all), as well as a panel of seven serine/threonine and 10 tyrosine kinases as well as one lipid kinase (IC50s = >200-500 µM), but does inhibit polo-like kinase 3 (PLK3, Ki = 7.2 µM) and Xenopus PLK1 (Plx1, IC50 = 10 µM). LFM-A13 increases anti-FAS antibody-induced apoptosis in NALM-6-UM-1 acute lymphoblastic leukemia (ALL) cells. It reduces tumor growth in an MMTV/neu transgenic mouse model of breast cancer when administered at a dose of 50 mg/kg.Formal Name: 2Z-cyano-N-(2,5-dibromophenyl)3-hydroxy-2-butenamide. CAS Number: 244240-24-2. Molecular Formula: C11H8Br2N2O2. Formula Weight: 360.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2)(1:2): 0.3 mg/ml, DMSO: 10 mg/ml. lambdamax: 219, 292 nm. SMILES: C/C(=C(\C#N)/C(=O)Nc1cc(Br)ccc1Br)/O. InChi Code: InChI=1S/C11H8Br2N2O2/c1-6(16)8(5-14)11(17)15-10-4-7(12)2-3-9(10)13/h2-4,16H,1H3,(H,15,17)/b8-6-. InChi Key: UVSVTDVJQAJIFG-VURMDHGXSA-N.