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AGI-5198

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    AGI-<wbr/>5198
  • AGI-<wbr/>5198
Cat No: 14624
Chemicals - Miscellaneous Chemicals
Cayman
€99.00
Price is excluding VAT and does not include packaging neither shipping

Selective inhibitor of IDH1 R132H and R132C mutants in vitro (IC50s = 0.07 and 0.16 µM, respectively) but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC50s > 100 μM); anti-tumor efficacy in vitro and in vivo; induces demethylation of histone H...

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Territorial Availability: Available through Bertin Pharma only in Europe
Product Overview:
Selective inhibitor of IDH1 R132H and R132C mutants in vitro (IC50s = 0.07 and 0.16 µM, respectively) but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC50s > 100 μM); anti-tumor efficacy in vitro and in vivo; induces demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation
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.
Size: 1 mg
Shipping: wet ice
Stability: Store at -20 degrees; shelf life 730 days maximum after production
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: 2903990000
UNSPSC code: 12352100

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.

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