Idasanutlin (RG7388)

Catalog No.S7205 Batch:S720503

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Technical Data

Formula

C31H29Cl2F2N3O4
Molecular Weight 616.48 CAS No. 1229705-06-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (162.21 mM)
Ethanol 1 mg/mL (1.62 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]
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 Assay:

[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 Study:

[1]
  • Animal Models

    Mice bearing SJSA human osteosarcoma xenografts

  • Dosages

    ~50 mg/kg daily

  • Administration

    p.o.

Selleck's Idasanutlin (RG7388) has been cited by 20 publications

Adipocyte p53 coordinates the response to intermittent fasting by regulating adipose tissue immune cell landscape [ Nat Commun, 2024, 15(1):1391] PubMed: 38360943
Synthetic lethality of combined ULK1 defection and p53 restoration induce pyroptosis by directly upregulating GSDME transcription and cleavage activation through ROS/NLRP3 signaling [ J Exp Clin Cancer Res, 2024, 43(1):248] PubMed: 39215364
Small molecule NMD and MDM2 inhibitors synergistically trigger apoptosis in HeLa cells [ Mol Cells, 2024, 47(7):100079] PubMed: 38871298
miR-16-5p enhances sensitivity to RG7388 through targeting PPM1D expression (WIP1) in Childhood Acute Lymphoblastic Leukemia [ Cancer Drug Resist, 2023, 6(2):242-256] PubMed: 37457129
miR-16-5p enhances sensitivity to RG7388 through targeting PPM1D expression (WIP1) in Childhood Acute Lymphoblastic Leukemia [ Cancer Drug Resist, 2023, 6(2):242-256] PubMed: 37457129
Genome-wide CRISPR/Cas9 screening for therapeutic targets in NSCLC carrying wild-type TP53 and receptor tyrosine kinase genes [ Clin Transl Med, 2022, 12(6):e882] PubMed: 35692096
Epstein Barr virus-positive B-cell lymphoma is highly vulnerable to MDM2 inhibitors in vivo [ Blood Adv, 2022, 6(3):891-901] PubMed: 34861697
FOXO1 Is a Key Mediator of Glucocorticoid-Induced Expression of Tristetraprolin in MDA-MB-231 Breast Cancer Cells [ Int J Mol Sci, 2022, 23(22)13673] PubMed: 36430156
Novel MDM2 Inhibitor XR-2 Exerts Potent Anti-Tumor Efficacy and Overcomes Enzalutamide Resistance in Prostate Cancer [ Front Pharmacol, 2022, 13:871259] PubMed: 35548335
p53 Regulates a miRNA-Fructose Transporter Axis in Brown Adipose Tissue Under Fasting [ Front Genet, 2022, 13:913030] PubMed: 35734423

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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