RG-7112

Catalog No.S7030 Batch:S703003

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Technical Data

Formula

C38H48Cl2N4O4S

Molecular Weight 726.28 CAS No. 939981-39-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (137.68 mM)
Ethanol 100 mg/mL (137.68 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.)

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Biological Activity

Description RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
Targets
MDM2 [1]
(Cell-free assay)
p53-MDM2 interaction [1]
(Cell-free assay)
11 nM(Kd) 18 nM
In vitro RG7112 is a potent and selective member of the nutlin family of MDM2 antagonists currently in phase I clinical studies. RG7112 binds MDM2 with high affinity (KD of 10.7 nM), blocking its interactions with p53 in vitro. A crystal structure of the RG7112–MDM2 complex reveals that the small molecule binds in the p53 pocket of MDM2, mimicking the interactions of critical p53 amino acid residues. Treatment of cancer cells expressing wild-type p53 with RG7112 activates the p53 pathway, leading to cell-cycle arrest and apoptosis. RG7112 shows potent antitumor activity against a panel of solid tumor cell lines. However, its apoptotic activity varies widely with the best response observed in osteosarcoma cells with MDM2 gene amplification. [1]
In vivo RG7112 activates p53 pathway and induces apoptosis in tumor cells in vivo. Oral administration of RG7112 to human xenograft-bearing mice at nontoxic concentrations caused dose-dependent changes in proliferation/apoptosis biomarkers as well as tumor inhibition and regression. Notably, RG7112 is highly synergistic with androgen deprivation in LNCaP xenograft tumors. [1]

Protocol (from reference)

Animal Study:

[1]

  • Animal Models

    SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice

  • Dosages

    25–200 mg/kg

  • Administration

    oral

Selleck's RG-7112 has been cited by 26 publications

The MDM2-p53 Axis Represents a Therapeutic Vulnerability Unique to Glioma Stem Cells [ Int J Mol Sci, 2024, 25(7)3948] PubMed: 38612758
Senolytic Combination Treatment Is More Potent Than Single Drugs in Reducing Inflammatory and Senescence Burden in Cells from Painful Degenerating IVDs [ Biomolecules, 2023, 13(8)1257] PubMed: 37627322
Senolytic Combination Treatment Is More Potent Than Single Drugs in Reducing Inflammatory and Senescence Burden in Cells from Painful Degenerating IVDs [ Biomolecules, 2023, 13(8)1257] PubMed: 37627322
Antagonizing MDM2 Overexpression Induced by MDM4 Inhibitor CEP-1347 Effectively Reactivates Wild-Type p53 in Malignant Brain Tumor Cells [ Cancers -Basel), 2023, 15(17)4326] PubMed: 37686602
Antagonizing MDM2 Overexpression Induced by MDM4 Inhibitor CEP-1347 Effectively Reactivates Wild-Type p53 in Malignant Brain Tumor Cells [ Cancers (Basel), 2023, 15(17)4326] PubMed: 37686602
Combined Mcl-1 and YAP1/TAZ inhibition for treatment of metastatic uveal melanoma [ Melanoma Res, 2023, 10.1097/CMR.0000000000000911] PubMed: 37467061
Multi-omics analysis reveals the mechanisms of action and therapeutic regimens of traditional Chinese medicine, Bufei Jianpi granules: Implication for COPD drug discovery [ Phytomedicine, 2022, 98:153963] PubMed: 35121390
Poroptosis: A form of cell death depending on plasma membrane nanopores formation [ iScience, 2022, 25(6):104481] PubMed: 35712073
Cell cycle block by p53 activation reduces SARS-CoV-2 release in infected alveolar basal epithelial A549-hACE2 cells [ Front Pharmacol, 2022, 13:1018761] PubMed: 36582523
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.