Product nameRG-7112, MDM2 inhibitor
DescriptionPotent, orally bioavailable MDM2 inhibitor
Potent, orally bioavailable MDM2 inhibitor that displays antineoplastic activity. Nutlin imidazoline compound. RG-7112 binds to MDM2, thereby preventing the binding of the MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. Binds MDM2 with KD = 10.7 nM. Blocks the p53- MDM2 interaction with an IC50 of 18 nM in HTRF assays.
Storage instructionsShipped at Room Temperature. Store at -20°C. It is important to note that this is air sensitive and impurities can occur as a result of air oxidation. Store In the Dark. Store under desiccating conditions.
DMSO 100 mg/mL (138 mM)
Ethanol 100 mg/mL (138 mM)
Insoluble in water
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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This product has been referenced in:
- Zhang Z et al. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem 22:4001-9 (2014). Read more (PubMed: 24997575) »
- Tovar C et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res 73:2587-97 (2013). Read more (PubMed: 23400593) »
- Vu B et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett 4:466-9 (2013). Read more (PubMed: 24900694) »