Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin with IC50 values of 90 and 40 nM, targeting the lipid kinase VPS34 with IC50 value of 19 nM in vitro. Autophinib targets VPS34 but not other lipid kinases, mTOR and TBK1. Autophinib appears to be ATP-competitive, targets VPS34 in cell lysate and induces cellular phenotypes consistent with VPS34 inhibition.
|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.
|Solubility||DMSO: ≥ 32 mg/mL|
Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34.
Robke L, et al. Angew Chem Int Ed Engl. 2017 Jul 3;56(28):8153-8157. PMID: 28544137.
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