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RG7112

Cat. No. M3628
RG7112 Structure
Synonym:

RO5045337

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 280 In stock
50mg USD 980 In stock
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Quality Control
Biological Activity

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 727.78
Formula C38H48Cl2N4O4S
CAS Number 939981-39-2
Purity 99.53%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 5. RG7112
Method gavage
Cell Lines MPM xenograft mouse
Concentrations 100 mg/Kg
Incubation Time days 1–21
Results The in vivo relevance of the combined actions of MDM2 inhibition and TRAIL agonists was tested using a xenograft mouse model that recapitulates sarcomatoid MPM with WT p53. Interestingly, our results demonstrated that RG7112 plus rhTRAIL significantly reduced tumor growth compared to the mock-treated group
Rating
References

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Vu B, et al. ACS Med Chem Lett. 2013 Apr 2;4(5):466-9. PMID: 24900694.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RG7112, RO5045337 supplier, Mdm2, inhibitors

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