NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. NSC-66811 induces p21, p53 and MDM2 accumulation in human colon cancer cells in vitro. NSC 66811 is more potent than the natural p53 peptide to bind with MDM2.
|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 20 mg/mL|
|Source||Acta Pharmacol Sin (2015). Figure 2. NSC 66811|
|Cell Lines||HepG2 cells|
|Concentrations||5 and 25 μmol/L|
|Incubation Time||24 h|
|Results||The p53 mRNA levels were up-regulated by NSC 66811 (Figure 2F) without affecting the CYP expression. NSC 66811 decreased the metabolism of DEM (Figure 2G) and TEST (Figure 2H) in a dose-dependent manner.|
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy.
Shangary S, et al. Annu Rev Pharmacol Toxicol. 2009;49:223-41. PMID: 18834305.
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.
Lu Y, et al. J Med Chem. 2006 Jun 29;49(13):3759-62. PMID: 16789731.
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