AZ628, 1 mg

This small molecule from STEMCELL Technologies is a quinazolinone that acts as a MEK/ERK pathway inhibitor. It inhibits several rapidly accelerated fibrosarcoma (RAF) kinases, including B-RAF, B-RAF V600E, and C-RAF-1, with in vitro kinase assay IC₅₀ values of 105, 34, and 29 nM respectively.

It strongly promotes B-RAF dimerization as a tight-binding inhibitor with a very slow off rate. Specificity profiling has shown that it also prevents activation of other tyrosine kinases, including vascular endothelial growth factor receptor 2 (VEGFR2), discoidin domain receptor 2 (DDR2), Lck/Yes Novel (LYN), feline McDonough sarcoma (FMS), and FMS-like tyrosine kinase 1 (FLT1).

In cancer research, this inhibitor reduces tumor growth, induces cell cycle arrest, and triggers apoptosis in a variety of cancer cell lines, particularly those carrying the B-RAF V600E mutation. It has a chemical formula of C₂₇H₂₅N₅O₂, a molecular weight of 451.5 g/mol, and is supplied as a crystalline solid of ≥98% purity. The product is stable as supplied for 12 months from the date of receipt and should be protected from prolonged exposure to light. Solubility has been confirmed in DMSO at ≤65 mM and in absolute ethanol at ≤0.5 mM. Stock solutions should be prepared fresh; for cell culture use, stock solution should be diluted into culture medium immediately before use, avoiding final DMSO concentrations above 0.1% due to potential cell toxicity. The compound has low solubility in aqueous media.