RG7112 (RO5045337) is the first-in-class 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
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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 |
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| 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 |
| Molecular Weight | 727.78 |
| Formula | C38H48Cl2N4O4S |
| CAS Number | 939981-39-2 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related Mdm2 Products |
|---|
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MMRi64 disrupts Mdm2-MdmX interactions. |
| MeOIstPyrd
MeOIstPyrd is an anti-skin cancer agent. |
| MDM2/XIAP-IN-3
MDM2/XIAP-IN-3 is a dual MDM2/XIAP inhibitor. |
| UNP-6457
UNP-6457 is a potent active MDM2-p53 interaction inhibitor with an IC50 values of 8.9 nM. |
| YL93
YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. |
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