AZD0424

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].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl

Src/Abl kinase inhibitor (SrcK-I), apoptosis[1]

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]. 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.

[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.