RG-7112

Catalog No.S7030 Synonyms: RO5045337

RG-7112 Chemical Structure

Molecular Weight(MW): 726.28

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.

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Cited by 3 publications

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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)
11 nM(Kd)
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]

Assay
Methods Test Index PMID
Western blot
MDM2 / PARP / Cleaved PARP; 

PubMed: 30022047     


U138MG, LN18, and A1207 cells were treated with RG7112 for 12 h at the indicated concentrations. p21, MDM2, p53, and PARP levels were examined by immunoblotting. Actin was used as a loading control. 

p-TP53 / PUMA / Survivin ; 

PubMed: 27659536     


Induction of TP53 phosphorylation and TP53 target proteins (TP21 and PUMA), as determined by western blotting. Cleaved PARP and survivin were also assessed to detect proapoptotic signaling

30022047 27659536
Immunofluorescence
p53 / p21; 

PubMed: 30022047     


An image-based immunofluorescence assay for p21 (green), p53 (red) and DAPI (blue) in A1207 cells treated with DMSO, RG7112 (2 μM), AMG232 (2 μM), and Camptothecin (10 μM) for 72 h are shown. 

30022047
Growth inhibition assay
Cell viability; 

PubMed: 30022047     


Cell numbers of U373MG, LN18, U251MG, A1207, DBTRG-05MG, and U87MG cells treated with different concentrations (0.07–54 μM) of RG7112.

30022047
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

Animal Research:

[1]
+ Expand
  • Animal Models: SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice
  • Formulation: 1% Klucel LF/0.1% Tween 80
  • Dosages: 25–200 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (137.68 mM)
Ethanol 100 mg/mL (137.68 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing. 		14mg/mL

* 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.

Chemical Information

Molecular Weight 726.28
Formula

C38H48Cl2N4O4S
CAS No. 939981-39-2
Storage powder
in solvent
Synonyms RO5045337

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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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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID