prt062607-p505-15-biib057-hcl

Description: PRT062607 (also known as P505-15, BIIB-057) HCl is a novel, potent, highly selective and orally bioavailable small molecule Syk inhibitor with potential anti-inflammatory activity. It inhibits Syk with an IC50 of 1 nM in cell-free assays, and shows > 80-fold selectivity for Syk over other kinases such as Fgr, Lyn, FAK, Pyk2 and Zap70. PRT062607produced excellent in vivo anti-inflammatory activity in two rodent modelsof rheumatoid arthritis. P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL. PRT062607effectively antagonize CLL cell survival after BCR triggering. Moreover, they inhibit the secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell transfer toward beneath stromal cells, the tissue homing chemokines CXCL13 and CXCL12.

References: J Pharmacol Exp Ther. 2012 Feb; 340(2):350-9; Leukemia. 2012 Jul; 26(7):1576-83.

Related CAS: 1370261-96-3 (free base); 1370261-97-4 (HCl);

Chemical Name: 4-((3-(2H-1, 2, 3-triazol-2-yl)phenyl)amino)-2-(((1R, 2S)-2-aminocyclohexyl)amino)pyrimidine-5-carboxamide hydrochloride

SMILES Code: O=C(C1=CN=C(N[CH]2[CH](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)N.[H]Cl