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编 号:F194176
分子式:C27H34N2O4
分子量:450.57
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1mg
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生物活性:
AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth.

体内研究:
AQX-435 (10 mg/kg; i.p.; 5 days) significantly reduced the volume of TMD8 tumors.AQX-435 (50 mg/kg; ip) inhibits DLBCL PDX tumors growth.AQX-435 reduced AKT phosphorylation and growth of DLBCL in vivo and cooperated with ibrutinib for tumor growth inhibition.Animal Model:NOD.Cg-Prkdc scidIl2rgtm1Wjl/SzJ mice (NSG mice) (TMD8 tumors)
Dosage:10 mg/kg
Administration:I.p.; in 7-day cycles each comprising 5 days of AQX-435 followed by 2 days with no drug
Result:Reduced the volume of TMD8 tumors.

体外研究:
AQX-435 reduces CLL cell viability in a dose-dependent manner.AQX-435-induced (5-30 μM; 24 hours) apoptosis is mediated via caspases since AQX435 induced PARP cleavage.AQX-435 effectively inhibits PI(3,4,5)P3-mediated signaling downstream of the BCR in CLL and DLBCL cells. AQX-435 and Ibrutinib combine effectively to enhanced inhibition of BCR signaling. AQX-435 induced TMD8 cell apoptosis in vitro with an IC50 of ~2 μM. AQX-435 reduces anti-IgM-induced AKT phosphorylation and induces apoptosis in DLBCL cells.
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