Nutlin-3a

Catalog No.S8059

Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.

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Nutlin-3a Chemical Structure

Nutlin-3a Chemical Structure
Molecular Weight: 581.49

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Product Information

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Product Description

Biological Activity

Description Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.
Targets p53/MDM2 interaction [3]
(Cell-free assay)
IC50 90 nM
In vitro Nutlin-3a displaces p53 from the binding pocket of MDM2 and thereby releases p53 from inhibition and proteasomal degradation, leading to induction of its downstream targets, cell cycle arrest, and apoptosis. Seven days of incubation with 10 μM nutlin-3a led to >90% inhibition of NIH3T3 cells’ growth[1]. Nutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner[1]. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments[1]. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHM cells after 40 h, which increased further after 60 h (85% and 65%, respectively) [1].
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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... Click to View More Cell Line Experimental Data

In vivo Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage [1]. Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors[1]. Tumors with wild-type p53 and mdm2 gene amplification will respond best to therapy with Nutlin-3a.
Features Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.

Protocol(Only for Reference)

Kinase Assay: [3]

Biacore studies Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel

Cell Assay: [2]

Cell lines OSA, T778, RMS13, U2OS, SaOS-2
Concentrations ~5 μM
Incubation Time 120 h
Method SRB

Animal Study: [1]

Animal Models SJSA-1 xenograft
Formulation 1% Klucel, 0.1% Tween 80
Dosages 50, 100, 200 mg/kg twice daily
Administration oral

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tovar C, et al. Proc Natl Acad Sci U S A, 2006, 103(6), 1888-1893.

[2] Ohnstad HO, et al. BMC Cancer, 2011, 11(211), 1-11.

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Chemical Information

Molecular Weight (MW) 581.49
Formula

C30H30Cl2N4O4

CAS No. 675576-98-4
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms (-)-Nutlin-3
Solubility (25°C) * In vitro DMSO 100 mg/mL (171.97 mM)
Ethanol 100 mg/mL (171.97 mM)
Water <1 mg/mL
In vivo 5% DMSO+55% PEG 300+ddH2O 8mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-Piperazinone, 4-[[(4S,5R)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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