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.
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纯度 |
>98%
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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.
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基本信息 | |
别名 |
PRT 060318 ,PRT060318,PRT 318,PRT-318,PRT318
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外观 |
Powder
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生物活性 | |
靶点 |
Syk
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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.
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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.
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分子结构图