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(±)-Nutlin-3 MDM2 antagonist, potent and selective

Catalog No.B6058
Size Price Stock Qty
5mg
$85.00
In stock
10mg
$160.00
In stock
50mg
$400.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

(±)-Nutlin-3

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Chemical Properties

Cas No. 548472-68-0 SDF Download SDF
Chemical Name 4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one
Canonical SMILES ClC1=CC=C(C=C1)C2N(C(N(C3)CCNC3=O)=O)C(C(C=CC(OC)=C4)=C4OC(C)C)=NC2C(C=C5)=CC=C5Cl
Formula C30H30Cl2N4O4 M.Wt 581.49
Solubility Soluble in DMSO Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
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.

Background

(±)-Nutlin-3 is a potent and selective MDM2 antagonist with IC50 value of 0.09 μM [1].

Mouse double minute 2 homolog (MDM2) is an important negative regulator of p53, a tumor suppressor. Disruption of the p53-MDM2 interaction can lead to the activation of p53 and tumor growth inhibition [1].

(±)-Nutlin-3 is a potent and selective MDM2 antagonist. In both normal and leukemic B cells, Nutlin-3 induced accumulation of p53 protein in a dose-dependent way. In B-CLL cells, Nutlin-3 also induced cell death with IC50 value of 10.4 μM and induced the transcription of p53 target genes, such as PCNA, CDKN1A/p21, GDF15, TNFRSF10B/TRAIL-R2, TP53I3/PIG3, GADD45, and DDB1 [2].

In mice bearing subcutaneous human cancer xenografts (SJSA-1), Nutlin-3 (200 mg/kg) orally treated twice a day for 20 days inhibited tumor growth by 90% [1]. In mice with established UKF-NB-3rDOX20 xenografts, Nutlin-3 (200 mg/kg) increased caspase-3 activity and induced apoptosis [3].

References:
Shinohara T, Uesugi M.  In-vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Tanpakushitsu Kakusan Koso. 2007 Oct;52(13 Suppl):1816-7.
Secchiero P, Barbarotto E, Tiribelli M, et al.  Functional integrity of the p53-mediated apoptotic pathway induced by the nongenotoxic agent nutlin-3 in B-cell chronic lymphocytic leukemia (B-CLL). Blood. 2006 May 15;107(10):4122-9.
Van Maerken T, Ferdinande L, Taildeman J, et al.  Antitumor activity of the selective MDM2 antagonist nutlin-3 against chemoresistant neuroblastoma with wild-type p53. J Natl Cancer Inst. 2009 Nov 18;101(22):1562-74.