AZ628, 10 mg

From STEMCELL Technologies, the MEK/ERK pathway inhibitor AZ628 is supplied as a crystalline solid. It is a quinazolinone that inhibits several rapidly accelerated fibrosarcoma (RAF) kinases, including B-RAF, B-RAF V600E, and C-RAF-1, with reported in vitro kinase assay IC₅₀ values of 105, 34, and 29 nM respectively. The compound strongly promotes B-RAF dimerization as a tight-binding inhibitor with a very slow off rate. Specificity profiling indicates that it also prevents activation of several 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).

The product has a reported purity of ≥ 98% and a molecular weight of 451.5 g/mol. It is stable at ≤20°C as supplied, should be protected from prolonged exposure to light, and remains stable for 12 months from date of receipt. Reported solubility limits are ≤ 65 mM in DMSO and ≤ 0.5 mM in absolute ethanol. The compound has low solubility in aqueous media. To prepare a 10 mM stock solution in DMSO, 1 mg should be resuspended in 221 μL of DMSO. For cell culture use, stock solution should be diluted into culture medium immediately before use, and final DMSO concentration should be kept below 0.1% due to potential cell toxicity.

In published cancer research applications, AZ628 has been reported to inhibit tumor growth, induce cell cycle arrest, and cause apoptosis in a variety of cancer cell lines, especially in lines with the B-RAF V600E mutation.