Idasanutlin (RG-7388)

For research use only.

Catalog No.S7205

5 publications

Idasanutlin (RG-7388) Chemical Structure

CAS No. 1229705-06-9

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.

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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 NFzDRm9EgXSxdH;4bYPDqGG|c3H5 NX76bpk1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0qVQUGgZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgdFU{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAyKM7:TR?= NYqydohtOjN6MEi1OFU>
HCT116 cells MYXDfZRwfG:6aXRCpIF{e2G7 M1XO[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCneIDy[ZN{cW6pIIfpcIQhfHmyZTDwOVMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgUXRVKGG|c3H5MEBKSzVyPUCuNFEh|ryP MVGyN|gxQDV2NR?=
SJSA1 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 MXGxJIg> NWLXd3V1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVlXSCrbnPvdpBwemG2aX;uJIFnfGW{IEGgbJIh[nliQ3zpZ4sucVRiRXTVJGhEWyCjc4PhfUBqdiCycnXz[Y5k\SCxZjCxNEUhcHWvYX6gd4VzfW1uIFnDOVA:OC5yNEWg{txO NFLSenEzPDR3NkS3Ni=>
SJSA1 cells MoLCR5l1d3SxeHnjxsBie3OjeR?= NIjjWnYyPiCq M{\oZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNLW0FzIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDF4IHjyd{BjgSCHZGWgbY5kd3Kyb4LheIlwdiCjc4PhfUBqdiCycnXz[Y5k\SCxZjCxNEUhcHWvYX6gd4VzfW1uIFnDOVA:OC5yNEWg{txO NHrFRZUzPDZyMU[0OC=>
RKO cells MnnvR5l1d3SxeHnjxsBie3OjeR?= Mn3zR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVmtQKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKHB3MzDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBjgSCPVGSgZZN{[XluIFnDOVA:OC5yNzFOwG0> MmjCNlM5ODh3NEW=
MDA-MB-435 cells MmrjR5l1d3SxeHnjxsBie3OjeR?= NYfzd5VPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{BmgHC{ZYPzbY5oKHB3MzDteZRidnRiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZpkhVVSWIHHzd4F6NCCLQ{WwQVkvOSEQvF2= NIPuZWgzOzhyOEW0OS=>
SW480 cells NHGwUIREgXSxdH;4bYPDqGG|c3H5 NXfLfHZuS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1d2OECgZ4VtdHNiZYjwdoV{e2mwZzDwOVMhdXW2YX70JIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1zMz6zJO69VQ>? NWPvOIRpOjN6MEi1OFU>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / MDM2 / Puma / Bax / Bak / Noxa / c-PARP-1; 

PubMed: 29232553     


Immunoblots showing the levels of indicated proteins in OCI-AML3 cells after treatment with 2 μM RG for indicated time. c-PARP-1, cleaved PARP-1 protein.

p21; 

PubMed: 29232553     


Immunoblots of p53 and p21 in OCI-AML3 cells after 24 hr treatment with indicated concentrations of RG.

EZH1 / H3K27me3; 

PubMed: 30596070     


H3K27me3 and EZH2 levels after treatment with different concentrations of GSK J4.

29232553 30596070
Immunofluorescence
E-cadherin; 

PubMed: 25671108     


Immunofluorescent microscopy of cells stained for E-cadherin (green) and DAPI (blue).

25671108
Growth inhibition assay
Cell viability; 

PubMed: 29857559     


Sensitivity of AML cells to idasanutlin. ell viability in AML cell lines treated for 24 h with increasing dosages of idasanutlin.

Cell proliferation; 

PubMed: 31238504     


Effect of GSK J4 on cell proliferation. Native and temozolomide (TMZ) resistant U251 (A), GBM3 (B), and DBTRG (C) glioblastoma cells were analyzed in parallel by MTS after 24 and 48 h of treatment with GSK J4 at different concentrations. Statistical analysis was performed by ANOVA, applying Bonferroni post-hoc correction. p-values: ** = 0.01; *** = 0.001; no asterisk indicates that the difference was not significant.

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

Kinase Assay:

[1]

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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]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Mice bearing SJSA human osteosarcoma xenografts
  • Dosages: ~50 mg/kg daily
  • Administration: p.o.
    (Only for Reference)

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+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
6.5mg/mL

* 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 Information

Molecular Weight 616.48
Formula

C31H29Cl2F2N3O4

CAS No. 1229705-06-9
Storage powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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

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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.

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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID