AGI-5198

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AGI-5198

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Cat No: 14624

Biochemicals - Small Molecule Inhibitors

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 ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[2-(cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide

Correlated keywords:

IDH-C35 IDHC35 IDH C35 inhibitors inhibits inhibitions isocitrates dehydrogenases IDH1 IDH-1 IDH 1 one ?-ketoglutarate 2OG 2 OG two 2-OG gliomas antitumor anti tumors anti-tumors 2-hydroxyglutarate hydroxyglutarates HGs 2-HG R132H mutants histones demethylations gliogenesis AGI5198 AGI 5198 potent selectives R132C in vitro TS603 TS-603 xenografts H3K9me3 genes gliogenic differentiations cancers enzymes activity actives metabolisms NADs NADPs NAD-dependent NADP-dependent dependents tricarboxylic acids cycles catalyzes oxidatives decarboxylations alpha ketoglutarates alpha-ketoglutarate carbons dioxides IDH1 IDH2 mutated mutations maps arginines residues catalytic pockets gains of functions NADPH-dependent NADPHs conversion AGI-5198 wild-type wilds types cells lines growths treatments periods induces expressions

Product Overview:
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.{22138} 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).{22135,22156,20681} 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).{23141} 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.{23140} 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.{23141} Under conditions of near complete 2-HG inhibition, AGI-5198 can induce demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.{23141}

Size	1 mg
Shipping	dry ice
CAS Number	1355326-35-0
Molecular Formula	C₂₇H₃₁FN₄O₂
SMILES	O=C(C(C1=C(C)C=CC=C1)N(C2=CC(F)=CC=C2)C(CN3C=CN=C3C)=O)NC4CCCCC4
Molecular Weight	462,6
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.