Home Apoptosis MDM2/MDMX inhibitor Idasanutlin (RG7388) For research use only.

Idasanutlin (RG7388)

Idasanutlin (RG7388) 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 (RG7388) Chemical Structure

Idasanutlin (RG7388) Chemical Structure

CAS: 1229705-06-9

Selleck's Idasanutlin (RG7388) has been cited by 17 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SJSA1 cells Cytotoxic assay Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.01 μM 23808545
HCT116 cells Cytotoxic assay Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.01 μM 23808545
SJSA1 cells Proliferation assay 1 h Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum, IC50=0.045 μM 24456472
SJSA1 cells Cytotoxic assay 16 h Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum, IC50=0.045 μM 24601644
RKO cells Cytotoxic assay Cytotoxicity against human RKO cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.07 μM 23808545
MDA-MB-435 cells Cytotoxic assay Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay, IC50=9.1 μM 23808545
SW480 cells Cytotoxic assay Cytotoxicity against human SW480 cells expressing p53 mutant assessed as growth inhibition by MTT assay, IC50=13.3 μM 23808545
Click to View More Cell Line Experimental Data

Biological Activity

Description Idasanutlin (RG7388) 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
p53-MDM2 interaction [1]
(Cell-free assay)
6 nM
In vitro
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot EZH1 / H3K27me3 p21 p53 / MDM2 / Puma / Bax / Bak / Noxa / c-PARP-1 30596070
Immunofluorescence E-cadherin 25671108
Growth inhibition assay Cell proliferation Cell viability 31238504
In Vivo
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]
Animal Research Animal Models Mice bearing SJSA human osteosarcoma xenografts
Dosages ~50 mg/kg daily
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05952687 Not yet recruiting Rhabdoid Tumor|Atypical Teratoid/Rhabdoid Tumor|Atypical Teratoid/Rhabdoid Tumor of CNS|CNS Tumor St. Jude Children''s Research Hospital January 2024 Phase 1
NCT03287245 Terminated Polycythemia Vera Hoffmann-La Roche February 21 2018 Phase 2
NCT03362723 Completed Solid Tumors Hoffmann-La Roche November 27 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 616.48 Formula

C31H29Cl2F2N3O4
CAS No. 1229705-06-9 SDF Download Idasanutlin (RG7388) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (162.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


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In vivo
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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.

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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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