BMS 986142

BMS 986142 is a Bruton's tyrosine kinase (BTK) inhibitor (IC50 = 0.5 nM). It is greater than 20-fold selective for BTK over a panel of 384 kinases. BMS 986142 inhibits calcium flux in Ramos B cells induced by B cell receptor (BCR) stimulation (IC50 = 9 nM), as well as BCR stimulation-induced proliferation of, and CD86 surface expression in, peripheral B cells (IC50s = 3 and 4 nM, respectively). It inhibits TNF-alpha production in human peripheral blood mononuclear cells (PBMCs) induced by Fcgamma receptor stimulation (IC50 = 3 nM). BMS 986142 (30 mg/kg per day) reduces the percentage of mice with severe proteinuria and increases survival in an NZB/W lupus-prone mouse model. It reduces hind paw tibiotarsal joint bone resorption and inflammation in a mouse model of collagen antibody-induced arthritis (CAIA) when administered at doses of 5 and 20 mg/kg.Formal Name: (2S,5R)-6-fluoro-5-[(3S)-3-(8-fluoro-1,4-dihydro-1-methyl-2,4-dioxo-3(2H)-quinazolinyl)-2-methylphenyl]-2,3,4,9-tetrahydro-2-(1-hydroxy-1-methylethyl)-1H-carbazole-8-carboxamide. CAS Number: 1643368-58-4. Molecular Formula: C32H30F2N4O4. Formula Weight: 572.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 15 mg/ml. lambdamax: 222 nm. SMILES: CC(C)(O)C(C1)CCC2=C1NC3=C2C(C4=CC=CC(N5C(N(C)C(C(F)=CC=C6)=C6C5=O)=O)=C4C)=C(F)C=C3C(N)=O. InChi Code: InChI=1S/C32H30F2N4O4/c1-15-17(7-6-10-24(15)38-30(40)19-8-5-9-21(33)28(19)37(4)31(38)41)25-22(34)14-20(29(35)39)27-26(25)18-12-11-16(32(2,3)42)13-23(18)36-27/h5-10,14,16,36,42H,11-13H2,1-4H3,(H2,35,39). InChi Key: ZRYMMWAJAFUANM-UHFFFAOYSA-N.