AGI-6780

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AGI-6780

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Cat No: 14639

Biochemicals - Small Molecule Inhibitors

Isocitrate dehydrogenases (IDHs) are NAD+ and NADP+-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing α-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide

Correlated keywords:

IDH inhibitors IDH2 isocitrate dehydrogenase ?-ketoglutarate 2-OG glioma anti-tumor 2-hydroxyglutarate 2-HG IDH1 R140Q mutant AML leukemias differentiations therapy cancers therapies AGI6780 AGIs 6780 AGI 6780 potent selective inhibits inhibitions two IDH-2 2 HGs U87 U-87 Us 87 TF-1 TF1 TFs 1 one cells growths suppresses slineages macrophages franulocytic

Product Overview:
Isocitrate dehydrogenases (IDHs) are NAD+ and NADP+-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing α-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-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.{23425} It binds allosterically at the dimer interface of mutant IDH2-R140Q, inhibiting 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 values of 11 and 18 nM, respectively.{23425} In primary human acute myelogenous leukemia cells, AGI-6780 suppressed cell growth and induced differentiation of immature blast cells toward macrophage and granulocytic lineages.{23245}

Size	1 mg
Shipping	dry ice
CAS Number	1432660-47-3
Molecular Formula	C₂₁H₁₈F₃N₃O₃S₂
SMILES	O=S(C1=CC(NC(NC2=CC=CC(C(F)(F)F)=C2)=O)=C(C3=CSC=C3)C=C1)(NC4CC4)=O
Molecular Weight	481,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2922.19
UNSPSC code	12352100

Technical File

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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.