Drug intelligence / Profile preview

AZ628

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

AZ628 is a potent, ATP-competitive small molecule inhibitor of Raf kinases, including B-Raf, B-Raf V600E, and C-Raf. It was developed by AstraZeneca as a targeted therapy to inhibit the MAPK/ERK signaling pathway, which is frequently dysregulated in various malignancies. While AZ628 has demonstrated significant preclinical activity in inhibiting the proliferation of BRAF-mutant melanoma and non-small cell lung cancer (NSCLC) cell lines, it is primarily utilized as a pharmacological research tool rather than a clinical candidate. Research involving AZ628 often focuses on understanding the molecular mechanisms of drug resistance and the behavior of drug-tolerant persister cells in cancer.

02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))CSF1R (Macrophage colony-stimulating factor receptor)DDR2 (Discoidin domain receptor tyrosine kinase 2)LYN (LYN proto-oncogene, Src family tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)

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