The selective mTORC1 complex inhibitor RMC-4529 is a bidentate inhibitor that has a rapamycin-derived, FKBP12-induced heterologous mTOR inhibitor covalently linked to an active-site (orthologous) inhibitor.
|Solubility (25°C)||DMSO ≥ 100 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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.
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Zederone, a germacrane-type sesquiterpene, has potently cytotoxic against human white blood cancer cells and human prostate cancer cells. Zederone significantly inhibits the proliferation and downregulates the protein expressions of mTOR, and phosphorylated p70 S6 kinase (p-p70s6K) in SKOV3 cells.
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