1. Metabolic Enzyme/Protease
    Apoptosis
  2. Phosphatase
    Apoptosis
  3. AQX-435

AQX-435 

目录号: HY-136268
产品使用指南

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。

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AQX-435 Chemical Structure

AQX-435 Chemical Structure

CAS No. : 1619983-52-6

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Description

AQX-435 is a potent SHIP1 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].

In Vitro

AQX-435 reduces CLL cell viability in a dose-dependent manner[1].
AQX-435 (5-30 µM; 24 hours)-induced apoptosis was 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: Chronic lymphocytic leukemia (CLL) cells
Concentration: 5-30 µM
Incubation Time: 24 hours
Result: Reduced CLL cell viability in a dose-dependent manner.
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.
Molecular Weight

450.57

Formula

C₂₇H₃₄N₂O₄

CAS No.

1619983-52-6

SMILES

O=C(C1=CC=CN=C1)N[C@@H]2C[C@@]3([H])C(C)(C)CCC[C@]3(C)[C@@H](C(C4=CC(O)=CC(O)=C4)=O)[C@@H]2C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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× = ×
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Keywords:

AQX-435AQX435AQX 435PhosphataseApoptosisB-cellchroniclymphocyticleukemiacaspasesPARPAKTphosphorylationInhibitorinhibitorinhibit

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产品名称:
AQX-435
目录号:
HY-136268
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