PRT-060318

PRT-060318CAS号: 1194961-19-7分子式: C18H24N6O分子量: 340.4描述纯度储存/保存方法别名外观靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
PRT-060318 is a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis ina transgenic mouse model.
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
PRT 060318 ,PRT060318,PRT 318,PRT-318,PRT318
外观
Powder
生物活性
靶点
Syk
In vitro(体外研究)
PRT318 is a potent inhibitor of purified Syk kinase with an IC50 of 4 nM. Syk kinase is inhibited by 92%, whereas all other kinases retains more than 70% at a concentration of 50 nM of PRT318. PRT318 and P505-15 effectively antagonize CLL cell survival after B-cell receptor (BCR) triggering and in nurse-like cell-co-cultures. They inhibit 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. PRT318 and P505-15 inhibit Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.
In vivo(体内研究)
PRT318 completely inhibits HIT immune complex-induced aggregation of both human and transgenic HIT mouse platelets. Pretreatment of mice with PRT318 markedly reduces HIT IC-induced thrombosis in the lungs. The Thrombosis Score is significantly lower for PRT318-treated mice compared with control.

分子结构图

PRT-060318