Name: Idasanutlin (RG7388)
Brand: Selleck Chemicals
SKU: S7205
Availability: InStock
Rating: 5 (23 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other MDM2/MDMX Inhibitors	Nutlin-3 Nutlin-3a RG-7112 Brigimadlin SAR405838 NSC 207895 NVP-CGM097 Siremadlin (HDM201) Nutlin-3b MX69

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (162.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.03mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	616.48	Formula	C₃₁H₂₉Cl₂F₂N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1229705-06-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Mechanism of Action

Targets/IC₅₀/Ki	p53-MDM2 interaction (Cell-free assay) 6 nM
In vitro	Idasanutlin (RG7388) 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.
Kinase Assay	Biochemical Binding Affinity – HTRF Assay
Kinase 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. Idasanutlin (RG7388) is stored in aliquots as a 10 mM stock solution 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.
In vivo	In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (RG7388) (25 mg/kg p.o.) causes tumor growth inhibition and regression. In a SJSA xenograft model, it results in induction of apoptosis and antiproliferation.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23808545/ [2] https://pubmed.ncbi.nlm.nih.gov/24812409/

Applications

Methods	Biomarkers	PMID
Western blot	p53 / MDM2 / Puma / Bax / Bak / Noxa / c-PARP-1 p21 EZH1 / H3K27me3	29232553
Immunofluorescence	E-cadherin	25671108
Growth inhibition assay	Cell viability Cell proliferation	29857559

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05952687	Withdrawn	Rhabdoid Tumor\|Atypical Teratoid/Rhabdoid Tumor\|Atypical Teratoid/Rhabdoid Tumor of CNS\|CNS Tumor	St. Jude Children''s Research Hospital	March 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

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Idasanutlin (RG7388) MDM2 Antagonist

Chemical Structure

Molecular Weight: 616.48