10074-G5 is an inhibitor of c-Myc-Max dimerization (IC50 =146 μM) that operates by binding and stabilizing c-Myc in its monomeric form. 10074-G5 inhibits c-Myc/Max heterodimer formation and its transcriptional activity. 10074-G5 is most efficient in inducing neuronal differentiation and lipid accumulation in MYCN-amplified neuroblastoma cells.
|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.
Discovery of Methyl 4'-Methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate, an Improved Small-Molecule Inhibitor of c-Myc-Max Dimerization.
Chauhan J, et al. ChemMedChem. 2014 Jun 27. PMID: 24976143.
Targeting of the MYCN Protein with Small Molecule c-MYC Inhibitors.
Müller I, et al. PloS one. 2014 May 23;9(5):e97285. PMID: 24859015.
In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization.
Clausen DM, et al. Journal of Pharmacology and Experimental Therapeutics. 2010 Dec;335(3):715-727. PMID: 20801893.
|Related c-Myc Products|
10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression.
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