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NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation. NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells. In nude mice bearing DLD-1 xenograft tumors, NSC59984 (45 mg/kg, i.p.) significantly represses tumor growth in a p73-dependent manner.
| 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.
| Molecular Weight | 265.27 |
| Formula | C12H15N3O4 |
| CAS Number | 803647-40-7 |
| Purity | >98% |
| Solubility | DMSO 50 mg/mL Ethanol 50 mg/mL |
| Storage | at -20°C |
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