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.
Drug Des Devel Ther. 2019 Jan 14;13:317-326.
YB-1 modulates the drug resistance of glioma cells by activation of MDM2/p53 pathway.
RG7112 purchased from AbMole
|Source||Oncotarget (2017). Figure 5. RG7112|
|Cell Lines||MPM xenograft mouse|
|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|
|Animal models||SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice|
|Formulation||1% Klucel LF/0.1% Tween 80|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 10 mM|
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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