Idasanutlin (RG-7388)

Catalog No.S7205

Idasanutlin (RG-7388) Chemical Structure

Molecular Weight(MW): 616.48

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.
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 MUPDfZRwfG:6aXRCpIF{e2G7 M1PyNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNLW0FzIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIIC1N{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNUDPxE1? M1zRPVI{QDB6NUS1
HCT116 cells MWnDfZRwfG:6aXRCpIF{e2G7 M2eyUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCneIDy[ZN{cW6pIIfpcIQhfHmyZTDwOVMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgUXRVKGG|c3H5MEBKSzVyPUCuNFEh|ryP NXzkfVRFOjN6MEi1OFU>
SJSA1 cells M3\hW3Bzd2yrZnXyZZRqd25iYYPzZZk> MYexJIg> NX35XI5iSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVlXSCrbnPvdpBwemG2aX;uJIFnfGW{IEGgbJIh[nliQ3zpZ4sucVRiRXTVJGhEWyCjc4PhfUBqdiCycnXz[Y5k\SCxZjCxNEUhcHWvYX6gd4VzfW1uIFnDOVA:OC5yNEWg{txO NV;Kd|hROjR2NU[0O|I>
SJSA1 cells NWn2RWJ[S3m2b4TvfIlkyqCjc4PhfS=> NVuyNmtJOTZiaB?= MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkAyPiCqcoOgZpkhTWSXIHnuZ49zeG:{YYTpc44h[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiMUClJIh2dWGwIIPldpVuNCCLQ{WwQVAvODR3IN88US=> Mn;tNlQ3ODF4NES=
RKO cells MWTDfZRwfG:6aXRCpIF{e2G7 MkD6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVmtQKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKHB3MzDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBjgSCPVGSgZZN{[XluIFnDOVA:OC5yNzFOwG0> NGDEVWEzOzhyOEW0OS=>
MDA-MB-435 cells NXnrOnlMS3m2b4TvfIlkyqCjc4PhfS=> Mkm5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczDlfJBz\XO|aX7nJJA2OyCvdYThcpQh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgUXRVKGG|c3H5MEBKSzVyPUmuNUDPxE1? M2TPcFI{QDB6NUS1
SW480 cells NEDwUFdEgXSxdH;4bYPDqGG|c3H5 MkTER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3c1QDBiY3XscJMh\XiycnXzd4lv\yCyNUOgcZV1[W62IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIJ6KE2WVDDhd5NigSxiSVO1NF0yOy5|IN88US=> MoTqNlM5ODh3NEW=

... Click to View More Cell Line Experimental Data

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]


Kinase Assay:


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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:


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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:


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  • Animal Models: Mice bearing SJSA human osteosarcoma xenografts
  • Formulation: Suspended in 1% Klucel LF/0.1% Tween 80
  • 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.

* 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


CAS No. 1229705-06-9
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03566485 Recruiting Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Estrogen Receptor-positive|HER2/Neu Negative Vanderbilt-Ingram Cancer Center|Genentech Inc.|Stand Up To Cancer June 25 2018 Phase 1|Phase 2
NCT03158389 Recruiting Glioblastoma Adult University Hospital Heidelberg|German Cancer Aid|German Cancer Research Center|National Center for Tumor Diseases Heidelberg May 7 2018 Phase 1|Phase 2
NCT03287245 Recruiting Polycythemia Vera Hoffmann-La Roche February 21 2018 Phase 2
NCT03362723 Active not recruiting Solid Tumors Hoffmann-La Roche November 27 2017 Phase 1
NCT03135262 Recruiting Follicular Lymphoma|Lymphoma Large B-Cell Diffuse Hoffmann-La Roche June 15 2017 Phase 1|Phase 2
NCT02828930 Completed Solid Tumors Hoffmann-La Roche September 8 2016 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