AQX-435 是一种有效的SHIP1 (SH2 domain-containing inositol-5′-phosphatase 1)激活剂。AQX-435 降低 B 细胞受体 (BCR) 下游 PI3K 活性，诱导恶性 B 细胞凋亡，减少淋巴瘤生长。
| 生物活性 | AQX-435 is a potentSHIP1phosphataseactivator. AQX-435 reducesPI3Kactivation downstream of the B-cell receptor (BCR) and inducesapoptosisof malignant B cells, and reduces lymphoma growth[1][2]. |
体外研究
(In Vitro) | AQX-435 reduces CLL cell viability in a dose-dependent manner[1].
AQX-435-induced (5-30 μM; 24 hours) apoptosis is mediated via caspases since AQX435 induced PARP cleavage[1].
AQX-435 effectively inhibits PI(3,4,5)P3-mediated signaling downstream of the BCR in CLL and DLBCL cells[1]. AQX-435 and Ibrutinib combine effectively to enhanced inhibition of BCR signaling. AQX-435 induced TMD8 cell apoptosis in vitro with an IC50of ~2 μM. AQX-435 reduces anti-IgM-induced AKT phosphorylation and induces apoptosis in DLBCL cells[1].
Cell Viability Assay[1] | Cell Line: | Chronic lymphocytic leukemia (CLL) cells | | Concentration: | 5-30 μM | | Incubation Time: | 24 hours | | Result: | Reduced CLL cell viability in a dose-dependent manner. |
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体内研究
(In Vivo) | AQX-435 (10 mg/kg; i.p.; 5 days) significantly reduced the volume of TMD8 tumors[1].
AQX-435 (50 mg/kg; ip) inhibits DLBCL PDX tumors growth[1].
AQX-435 reduced AKT phosphorylation and growth of DLBCL in vivo and cooperated with ibrutinib for tumor growth inhibition[1].
| Animal Model: | NOD.Cg-Prkdc scidIl2rgtm1Wjl/SzJ mice (NSG mice) (TMD8 tumors)[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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