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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