PRT062607 (P505-15) HCl

InformationPRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.In vitroPRT062607(P505-15) anti-SYK activity is at least 80-fold greater than its affinity for other kinases. at least 80-fold greater than its affinity for other kinases. PRT062607 potently inhibits B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM). PRT062607 inhibits BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT062607 furthermore inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.In vivoThe pharmacokinetic/pharmacodynamic relationship predicted that 70% Syk suppression is maintained in mice over a 24h period after 30 mg/kg dosing. At 15 mg/kg, Syk inhibition ranges from 7.5% (Cmin) to 78.4% (Cmax) with an average inhibition of 67% over 24 h. Oral administration of PRT062607 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. Statistically significant efficacy is observed at concentrations that specifically suppressed Syk activity by 67%.Cell Datacell lines：Calu-3 and A-549 cell linesConcentrations：~6 μMIncubation Time：3 daysPowder Purity:≥98%.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C19H23N9O·HCl

Molecular Weight: 429.91