AZD0424

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AZD0424 

AZD0424 是选择性 Src/Abl 激酶抑制剂，可口服，具有抗肿瘤活性。AZD0424 可以诱导淋巴瘤细胞凋亡 (apoptosis) 和细胞周期停滞。

AZD0424

AZD0424 Chemical Structure

CAS No. : 692054-06-1

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生物活性

AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity[1]. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells[2].

IC50 & Target

Src/Abl kinase inhibitor (SrcK-I), apoptosis[1]
体外研究
(In Vitro)

AZD0424 (1-5 μM; 24-48 hours) is emerged to be the more effective of the three tested inhibitors (AZM559756, AZD0530 and AZD0424), inducing the highest levels of apoptosis with the lowest concentrations in lymphoma cells[2].
AZD0424 (5 μM; 48 hours) leads to increased G0/G1 cell cycle arrest in DOHH-2 and WSU-NHL cells, whereas the cell cycle progression of the nonsensitive cell lines Raji and Jurkat remains unaffected[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: DOHH-2, WSU-NHL, Raji, Jurkat, Karpas-299 and HUT78 cells
Concentration: 1 μM; 2 μM; 3 μM; 4 μM; 5 μM;
Incubation Time: 24 hours, 48 hours
Result: Induced apoptosis in lymphoma cells.

Cell Cycle Analysis[2]

Cell Line: DOHH-2, WSU-NHL, Raji and Jurkat cells
Concentration: 1 μM; 2 μM; 3 μM; 4 μM; 5 μM;
Incubation Time: 48 hours
Result: Increased G0/G1 cell cycle arrest in DOHH-2 and WSU-NHL cells.

Clinical Trial

分子量

528.99

Formula

C25H29ClN6O5
CAS 号

692054-06-1
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.
参考文献

  • [1]. Woodcock VK, et al. A first-in-human phase I study to determine the maximum tolerated dose of the oral Src/ABL inhibitor AZD0424. Br J Cancer. 2018 Mar 20;118(6):770-776.

    [2]. Nowak D, et al. Src kinase inhibitors induce apoptosis and mediate cell cycle arrest in lymphoma cells. Anticancer Drugs. 2007 Oct;18(9):981-95.

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