Description
Nutlin-3 is a small-molecule inhibitor of mouse double minute 2 (MDM2) with IC50 value of 0.09 μM.
Product Overview
Nutlin-3 is a small-molecule inhibitor of MDM2 (mouse double minute 2) with IC50 value of 0.09μM. Nutlin-3 binds MDM2 in the TP53-bindingpocket, thereby interfering with MDM2-directed TP53 degradation. This has been shown to cause cell cycle arrest, growth inhibitionand apoptosis in both solid tumors and lymphoid neoplasms. In mantle cell lymphoma(MCL), it is reported that Nutlin-3 can inhibit cell growth and activate apoptosis in bothwt-TP53 (IC50 of 1 to 10μM) and mt-TP53 (IC50 of 22.5μM) cells. Nutlin-3 can also effectcell cycle in gastric cancer cell lines. It induces G1 arrest inMKN-45 and SNU-1 cell lines. In vitro assay shows Nutlin-3can enhance the antitumoreffects of conventional chemotherapeutic agents in several gastric cancer cell lines. And in in vivo assay, Nutlin-3 significantly inhibits the growth of xenograft tumors.
Synonyms
Nutlin-3a; Nutlin 3a
Molecular Formula
C30H30Cl2N4O4
Chemical Name
4-[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request