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Nutlin-3a chiral
MDM2 inhibitor, antiproliferative and antiproapoptotic

Nutlin-3a chiral

Catalog No. A3671
Size Price Stock Qty
10mg $120.00 In stock
50mg $580.00 In stock
200mg $1,980.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Nutlin-3a chiral

Related Biological Data

Nutlin-3a chiral

Related Biological Data

Nutlin-3a chiral

Biological Activity

Description Nutlin-3 is a small-molecule inhibitor of mouse double minute 2 (MDM2) with IC50 value of 0.09 μM.
Targets MDM2          
IC50 0.09 μM          

Nutlin-3a chiral Dilution Calculator

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Chemical Properties

Cas No. 675576-98-4 SDF Download SDF
Synonyms Nutlin-3a;Nutlin 3a
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
Canonical SMILES CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
Formula C30H30Cl2N4O4 M.Wt 581.49
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Nutlin-3 is a small-molecule inhibitor of MDM2 (mouse double minute 2) with IC50 value of 0.09μM [1].

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 [2].

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 [3].

References:
[1] Lyubomir T.Vassilev et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.Science.2004, 303: 844-848.
[2] Yoko Tabe, Denise Sebasigari, Linhua Jin, et al.MDM2 Antagonist Nutlin-3 Displays Antiproliferative andProapoptotic Activity in Mantle Cell Lymphoma. Clin Cancer Res. 2009, 15:933-942.
[3] Shinji Endo,Kenji Yamato,Sachiko Hirai,Toshikazu Moriwaki,Kuniaki Fukuda,Hideo Suzuki,Masato Abei,Ichiro Nakagawa and IchinosukeHyodo.Potent in vitro and in vivo antitumor effects ofMDM2 inhibitor nutlin-3 in gastric cancer cells.Cancer Science. 2011, 102 (3): 605-613.