|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
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.) |
||||
Preparing Stock Solutions
Biological Activity
| Description | RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM. | ||||
|---|---|---|---|---|---|
| Targets |
|
||||
| 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: |
|
|---|
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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.