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AQX-435

目录号 : GC70759

AQX-435是一种强效的SHIP1磷酸酶激活剂。

AQX-435 Chemical Structure

Cas No.:1619983-52-6

规格 价格 库存 购买数量
1 mg
¥6,750.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

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].

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].

References:
[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.

Chemical Properties

Cas No. 1619983-52-6 SDF
分子式 C27H34N2O4 分子量 450.57
溶解度 DMSO : 100 mg/mL (221.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2194 mL 11.0971 mL 22.1941 mL
5 mM 0.4439 mL 2.2194 mL 4.4388 mL
10 mM 0.2219 mL 1.1097 mL 2.2194 mL
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