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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Metabolism >Dehydrogenase Inhibitor >N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide

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

N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide Structure
  • ₹12946.7 - ₹52198.15
  • Product name: N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide
  • CAS: 1355326-35-0
  • MF: C27H31FN4O2
  • MW: 462.56
  • EINECS:806-071-1
  • MDL Number:MFCD24848688
  • Synonyms:AGI-5198 (IDH-C35);N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide;IDH-C35 /IDHC35;N-CYCLOHEXYL-2-(N-(3-FLUOROPHENYL)-2-(2-METHYL-1H-IMIDAZOL-1-YL)ACETAMIDO)-2-(O-TOLYL)ACETAMIDE;AGI5198;IDH-C35 /IDHC35;IDH C35;IDH-C35;AGI5198;N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide
2 prices
Selected condition:

Brand

  • Sigma-Aldrich(India)

Package

  • 5MG
  • 25MG
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML0839
  • Product descriptionAGI-5198 ≥98% (HPLC)
  • Packaging5MG
  • Price₹12946.7
  • Updated2022-06-14
  • Buy
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML0839
  • Product descriptionAGI-5198 ≥98% (HPLC)
  • Packaging25MG
  • Price₹52198.15
  • Updated2022-06-14
  • Buy
Manufacturer Product number Product description Packaging Price Updated Buy
Sigma-Aldrich(India) SML0839 AGI-5198 ≥98% (HPLC) 5MG ₹12946.7 2022-06-14 Buy
Sigma-Aldrich(India) SML0839 AGI-5198 ≥98% (HPLC) 25MG ₹52198.15 2022-06-14 Buy

Properties

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 Information

Symbol(GHS): GHS hazard pictograms
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H301 Toxic if swalloed Acute toxicity,oral Category 3 Danger GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
Precautionary statements:
P301+P310 IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Description

Isocitrate dehydrogenases (IDHs) are nicotinamide adenine dinucleotide (NAD+) and NAD phosphate (NADP+)-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing a-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas. The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG). AGI-5198 is a potent, selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16 μM, respectively, but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC50s > 100 μM). 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 and 0.07 μM, respectively. 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.

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