Cis-imidazoline analog that inhibits the interaction between p53 and its negative regulator MDM2 (IC50 = 0.09 μM). It induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53, but not in cells with mutated p53. Nutlin-3 also inhibits the growth of human tumor xenografts in nude mice by 90% at a dose of 200 mg/kg.

(±)–4–[4,5–Bis(4–chlorophenyl)–2–(2–isopropoxy–4–methoxy–phenyl)–4,5–dihydro–imidazole–1–carbonyl]–piperazin–2–one

>98% by TLC.

Soluble in DMSO (50 mg/ml)

White crystalline solid

Useful as an MDM2 antagonist, as a p53 activator and as an apoptosis inducer.

1. Vassilev L.T. et al. In vivo activation of the p53 pathway by small -molecule antagonists of MDM2. Science 2004. 303(5659):844.

Protect from light. Protect from moisture. Avoid freeze/thaw cycles.

Protease

Inhibitors/Activators