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.
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Source | Acta Pharmacol Sin (2015). Figure 2. NSC 66811 |
| Method | PCR | |
| 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. |
| Molecular Weight | 340.42 |
| Formula | C23H20N2O |
| CAS Number | 6964-62-1 |
| Solubility (25°C) | DMSO 40 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.
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