| Bioactivity | 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[1][2]. |
| Invitro | 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 IC50 of ~2 µM. AQX-435 reduces anti-IgM-induced AKT phosphorylation and induces apoptosis in DLBCL cells[1]. Cell Viability Assay[1] Cell Line: |
| 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: |
| Name | AQX-435 |
| CAS | 1619983-52-6 |
| Formula | C27H34N2O4 |
| Molar Mass | 450.57 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Lyoyd F. MACKENZIE, et al. Ship1 modulators and methods related thereto.WO2014110036A1. [2]. Lemm EA, et al. Preclinical Evaluation of a Novel SHIP1 Phosphatase Activator for Inhibition of PI3K Signaling in Malignant B Cells. Clin Cancer Res. 2020;26(7):1700-1711. |