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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.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Sovleplenib  |  Syk Kinase Peptide Substrate  |  Cevidoplenib dimesylate  |  Syk-IN-4  |  Syk Inhibitor II dihydrochloride dihydrate  |  GSK143 dihydrochloride  |  Syk-IN-6  |  PRT062607 Hydrochloride  |  MNS  |  TAK-659 hydrochloride  |  Gusacitinib hydrochloride  |  Dehydroabietinol  |  R406 free base  |  Lanraplenib  |  Fostamatinib Disodium  |  Syk Kinase Peptide Substrate, Biotin labeled  |  BAY 61-3606 dihydrochloride  |  SYK/JAK-IN-1  |  Cerdulatinib hydrochloride  |  TAS05567  |  SRX3207  |  Entospletinib  |  GSK2646264  |  Syk-IN-3  |  R112

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