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AGI-5198 | R132 mutant isocitrate dehydrogenase inhibitor

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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Catalog#  10-4599

$70.00
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CAS:
1355326-35-0
Catalog Number:
10-4599
Activity:
R132 mutant isocitrate dehydrogenase inhibitor
Chemical Name:
N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide
Molecular Weight:
462.56
Molecular Formula:
C27H31FN4O2
Solubility:
Soluble in DMSO (up to 10 mg/ml) or in Ethanol (up to 5 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethsnol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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