Idasanutlin (RG-7388)

Catalog No.S7205

For research use only.

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.

Idasanutlin (RG-7388) Chemical Structure

CAS No. 1229705-06-9

Selleck's Idasanutlin (RG-7388) has been cited by 9 Publications

Purity & Quality Control

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Biological Activity

Description Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.
Targets
Mdm2 [1]
(Cell-free assay)
6 nM
In vitro

Idasanutlin inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SJSA1 cells MVrDfZRwfG:6aXRCpIF{e2G7 MkfHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2pUSTFiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGVicEWzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1yLkCxJO69VQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhyOEW0OUc,OjN6MEi1OFU9N2F-
HCT116 cells NVHKOFRlS3m2b4TvfIlkyqCjc4PhfS=> MnzHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIIC1N{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNUDPxE1? M4TTc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEC4OVQ2Lz5{M{iwPFU1PTxxYU6=
SJSA1 cells NXzQ[FkxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYqxJIg> NXPMfmc2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVlXSCrbnPvdpBwemG2aX;uJIFnfGW{IEGgbJIh[nliQ3zpZ4sucVRiRXTVJGhEWyCjc4PhfUBqdiCycnXz[Y5k\SCxZjCxNEUhcHWvYX6gd4VzfW1uIFnDOVA:OC5yNEWg{txO M{[3dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEW2OFczLz5{NES1OlQ4OjxxYU6=
SJSA1 cells MoTVR5l1d3SxeHnjxsBie3OjeR?= NFf6fFYyPiCq MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkAyPiCqcoOgZpkhTWSXIHnuZ49zeG:{YYTpc44h[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiMUClJIh2dWGwIIPldpVuNCCLQ{WwQVAvODR3IN88US=> NVHJUY5ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NFE3PDRpPkK0OlAyPjR2PD;hQi=>
RKO cells NYXXbGU4S3m2b4TvfIlkyqCjc4PhfS=> MorVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVmtQKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKHB3MzDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBjgSCPVGSgZZN{[XluIFnDOVA:OC5yNzFOwG0> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhyOEW0OUc,OjN6MEi1OFU9N2F-
MDA-MB-435 cells MmHPR5l1d3SxeHnjxsBie3OjeR?= NH75UWhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFM2KGOnbHzzJIV5eHKnc4PpcocheDV|IH31eIFvfCCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDifUBOXFRiYYPzZZktKEmFNUC9PU4yKM7:TR?= NGXEOW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iwPFU1PSd-MkO4NFg2PDV:L3G+
SW480 cells NHLaVmZEgXSxdH;4bYPDqGG|c3H5 Mn\qR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3c1QDBiY3XscJMh\XiycnXzd4lv\yCyNUOgcZV1[W62IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIJ6KE2WVDDhd5NigSxiSVO1NF0yOy5|IN88US=> NVzP[5E3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4NFg2PDVpPkKzPFA5PTR3PD;hQi=>
Assay
Methods Test Index PMID
Western blot p53 / MDM2 / Puma / Bax / Bak / Noxa / c-PARP-1 ; p21 ; EZH1 / H3K27me3 29232553 30596070
Immunofluorescence E-cadherin 25671108
Growth inhibition assay Cell viability ; Cell proliferation 29857559 31238504
In vivo In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. [1] In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation. [2]

Protocol (from reference)

Kinase Assay:

[1]

  • Biochemical Binding Affinity – HTRF Assay:

    The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient.

Cell Research:

[1]

  • Cell lines: wt-p53 cancer cell lines (SJSA1, RKO, HCT116)
  • Concentrations: ~10 μM
  • Incubation Time: 24 hours
  • Method:

    Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition.

Animal Research:

[1]

  • Animal Models: Mice bearing SJSA human osteosarcoma xenografts
  • Dosages: ~50 mg/kg daily
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(162.21 mM)
Ethanol 8 mg/mL warmed
(12.97 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

1.25mg/mL

Chemical Information

Molecular Weight 616.48
Formula

C31H29Cl2F2N3O4

CAS No. 1229705-06-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)CC1C(C(C(N1)C(=O)NC2=C(C=C(C=C2)C(=O)O)OC)C3=C(C(=CC=C3)Cl)F)(C#N)C4=C(C=C(C=C4)Cl)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03287245 Terminated Drug: Idasanutlin Polycythemia Vera Hoffmann-La Roche February 21 2018 Phase 2
NCT03362723 Completed Drug: Idasanutlin Solid Tumors Hoffmann-La Roche November 27 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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