Ivosidenib is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG).
In vitro, TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.Treatment with AG-120 decreases intracellular 2-HG levels, inhibites growth factor independent proliferation and restores erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells.
|Cell lines||TF-1 cells|
|Preparation method||TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.|
|Concentrations||0.5, 1.0, and 5.0 μM|
|Incubation time||6 days|
|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: ≥ 60 mg/mL|
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
Popovici-Muller J, et al. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. PMID: 29670690.
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