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.
|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 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.
|Solubility||DMSO 50 mg/mL
Ethanol 50 mg/mL
Small-Molecule NSC59984 Restores p53 Pathway Signaling and Antitumor Effects against Colorectal Cancer via p73 Activation and Degradation of Mutant p53.
Zhang S, et al. Cancer Res. 2015 Sep 15;75(18):3842-52. PMID: 26294215.
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