AGI-5198 | R132 mutant isocitrate dehydrogenase inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 5 mg | $40.00 | ||
| 25 mg | $95.00 |
AGI-5198 (135526-35-0) is a potent (IC50 = 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1).1 It is selective for the R132H-IDH1 mutant and does not affect wild type cells.2 This mutation results in loss-of-function for oxidative decarboxylation of isocitrate and gain-of-function for production of the oncometabolite R-2-hydroxyglutarate (R-2HG) from alpha-ketoglutarate (2-OG).
References/Citations:
1) Popovici-Muller et al. (2012), Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG In Vivo; ACS Med. Chem. Lett., 3 850
2) Rohle et al. (2013), An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells; Science, 340 626
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
AGI-5198 (135526-35-0) is a potent (IC50 = 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1).1 It is selective for the R132H-IDH1 mutant and does not affect wild type cells.2 This mutation results in loss-of-function for oxidative decarboxylation of isocitrate and gain-of-function for production of the oncometabolite R-2-hydroxyglutarate (R-2HG) from alpha-ketoglutarate (2-OG).
References/Citations:
1) Popovici-Muller et al. (2012), Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG In Vivo; ACS Med. Chem. Lett., 3 850
2) Rohle et al. (2013), An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells; Science, 340 626
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1-855-FOCUS21
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