IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species and achieves significant in vivo efficacy with daily oral dosing of 10-25 mg/kg.
|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 ≥ 30 mg/mL|
IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities
Marina P, et al. AACR; Cancer Res. 2015 Aug;Volume 75, Issue 15 Supplement, pp. 4380.
cGAMP is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA.
N6-isopentenyladenosine is a plant hormone.
X-α-Gal is suitable as a substrate for α-galactosidase.
RU320521 (also known as RU521; RU.521) is a potent and selective inhibitor of cGAS, inhibiting cGAS-mediated interferon upregulation.
|Dextran sulfate sodium salt
Dextran sulfate sodium salt is a polyanionic derivative of dextran produced by esterification of Dextran with chlorosulphonic acid.
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