BIIB-057

BIIB-057 is a potent inhibitor of the non-receptor tyrosine kinase Syk (IC50 = 1 nM). It displays at least 80-fold selectivity for Syk over other kinases. BIIB-057 blocks B cell receptor-mediated cell signaling and activation in whole blood (IC50s = 0.27 and 0.28 µM, respectively), as well as Fc? receptor 1-mediated basophil degranulation (IC50 = 0.15 µM). It antagonizes chemokine production, cell migration, and survival of chronic lymphocytic leukemia (CLL) cells after B cell receptor activation and synergistically enhances the action of fludarabine (Cay-14128) in killing CLL cells. BIIB-057 is orally bioavailable, as it produces dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. It also prevents splenomegaly and inhibits non-Hodgkin lymphoma tumor growth in a xenograft model.Formal Name: 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-5-pyrimidinecarboxamide. CAS Number: 1370261-96-3. Synonyms: P505-15, PRT062607, PRT2607. Molecular Formula: C19H23N9O. Formula Weight: 393.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 25 mg/ml, Ethanol: 10 mg/ml. lambdamax: 264 nm. SMILES: NC(C(C=NC(N[C@@H]1CCCC[C@@H]1N)=N2)=C2NC3=CC(N4N=CC=N4)=CC=C3)=O. InChi Code: InChI=1S/C19H23N9O/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28/h3-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27)/t15-,16+/m0/s1. InChi Key: TXGKRVFSSHPBAJ-JKSUJKDBSA-N.