N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide Property

Boiling point:

707.6±60.0 °C(Predicted)

Density 

1.21±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble3mg/mL, clear

form 

powder

pka

14.02±0.20(Predicted)

color 

white to beige

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

InChIKey

FNYGWXSATBUBER-UHFFFAOYSA-N

Safety

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

45

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide Chemical Properties,Usage,Production

Description

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).

Uses

AGI5198 inhibits mutant IDH1 (isocitrate dehydrogenase 1) in cancer cells which delays growth and promotes differentiation of the glioma cells.

Uses

AGI-5198 has been used as a negative control in ligand dilution series.

Biochem/physiol Actions

In human chondrosarcoma cell line JJ012, AGI-5198 promotes apoptosis and G2/M cell cycle arrest. It also prevents the generation of colony in chondrosarcoma cell lines. AGI-5198 hinders the multiplication of cell and induces demethylation of H3K9me3 and H3K27me3.

target

R132H-IDH1

storage

Store at -20°C

References

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