RN-486

RN-486 is a Bruton's tyrosine kinase inhibitor (Kd = 0.31 nM, IC50 = 4 nM) that displays a high degree of selectivity when tested against a panel of 369 kinases. It has been shown to block Fcepsilon receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcgamma receptor engagement-mediated TNF-alpha production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of CD69 in B cells whole blood (IC50 = 21 nM). RN-486 is reported to produce anti-inflammatory and bone-protective effects in mouse collagen-induced arthritis and rat adjuvant-induced arthritis models.Formal Name: 6-cyclopropyl-2-[3-[1,6-dihydro-1-methyl-5-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-6-oxo-3-pyridinyl]-2-(hydroxymethyl)phenyl]-8-fluoro-1(2H)-isoquinolinone. CAS Number: 1242156-23-5. Molecular Formula: C35H35FN6O3. Formula Weight: 606.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.2 mg/ml, DMSO: 0.2 mg/ml. lambdamax: 213, 217, 294, 344 nm. SMILES: O=C1C2=C(F)C=C(C3CC3)C=C2C=CN1C4=CC=CC(C5=CN(C)C(C(NC6=NC=C(N7CCN(C)CC7)C=C6)=C5)=O)=C4CO. InChi Code: InChI=1S/C35H35FN6O3/c1-39-12-14-41(15-13-39)26-8-9-32(37-19-26)38-30-18-25(20-40(2)34(30)44)27-4-3-5-31(28(27)21-43)42-11-10-23-16-24(22-6-7-22)17-29(36)33(23)35(42)45/h3-5,8-11,16-20,22,43H,6-7,12-15,21H2,1-2H3,(H,37,38). InChi Key: ZTUJNJAKTLHBEX-UHFFFAOYSA-N.