PRT-060318

价格： ￥384 - 7920

品牌：MedChemExpress(MCE) 品牌认证

货号：HY-12974

产品详情

PRT-060318

CAS No. : 1194961-19-7

MCE 国际站：PRT-060318

产品活性：PRT-060318 (PRT318)是新颖选择性的酪氨酸激酶 (Syk) 抑制剂， IC₅₀值为4 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Syk

In Vitro: 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: 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.