AGI-5198 (also know as IDH-C35) is a potent and selective mutant IDH1 inhibitor. AGI-5198 has been shown to have anti-tumor efficacy in the TS603 glioma cell line and to lower tumor 2-HG production in HT1080 and U87MG cells with IC50 values of 0.48 μM and 0.07 μM, respectively. AGI-5198 (IDH-C35) inhibits IDH1 R132H mutant and R132C mutant in vitro with IC50 of 0.07 μM and 0.16 μM respectively, but not wild-type IDH1 or any of the examined IDH2 isoforms (IC50 > 100 μM). In R132H-IDH1 glioma xenografts, AGI-5198 (450 mg/kg/day) caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts. Under conditions of near complete 2-HG inhibition, AGI-5198 can induce demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.
|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.
An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.
Rohle D, et al. Science. 2013 May 3;340(6132):626-30. PMID: 23558169.
|Related Dehydrogenase Products|
Trilostane is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.
Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.
Vidofludimus is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH.
ML323 is a highly potent and selective USP1-UAF1 inhibitor with IC50 of 76 nM.
MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.