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AGI-5198

Catalog No. T2104   CAS 1355326-35-0
Synonyms: IDH-C35

AGI-5198 (IDH-C35) is a highly effective and specific inhibitor of IDH1 R132H/R132C mutants (IC50: 0.07/0.16 μM).

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AGI-5198 Chemical Structure
AGI-5198, CAS 1355326-35-0
Pack Size Availability Price/USD Quantity
5 mg In stock $ 32.00
10 mg In stock $ 52.00
50 mg In stock $ 77.00
100 mg In stock $ 126.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 99.23%
Purity: 97.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AGI-5198 (IDH-C35) is a highly effective and specific inhibitor of IDH1 R132H/R132C mutants (IC50: 0.07/0.16 μM).
Targets&IC50 R132H-IDH1:70 nM, R132C-IDH1:0.16 μM
Kinase Assay IDH enzyme activity: Compound is prepared as 10 mM stock in DMSO and diluted to 50X final concentration in DMSO, for a 50 μL reaction mixture. IDH enzyme activity converting alpha-ketogluta rate to 2-hydroxyglutarate is measured using a NADPH depletion assay. In the assay the remaining cofactor is measured at the end of the reaction with the addition of a catalytic excess of diaphorase and resazurin, to generate a fluorescent signal in proportion to the amount of NADPH remaining. IDH enzyme activity in the direction of isocitrate to alpha-ketoglutarate conversion is measured by direct coupling of the NADPH production to conversion of resazurin to resorufin by diaphorase. In both cases, resorufin is measured fluorometrically at Ex544 Em 590.
Cell Research AGI-5198 is dissolved in DMSO.TS603 cells are grown in medium containing either AGI-5198 (1.5 μM) or DMSO vehicle control.One week prior to harvest cells are ransferred to differentiation medium (DMEM F12; 15 mM HEPES; 0.06% glucose; B27 without vitamin A; N2; Insulin/transferrin; 1% FBS) containing freshly added retinoic acid (1 μM).ChIP of non-crosslinked cells is then carried out using established ChIP methods.350 μg of lysate is immunoprecipitated-using anti-H3K9Me3,H3K27me3 or Rabbit Control IgG.After washing,ChIP DNA is eluted from protein G beads and analyzed by RT-PCR using SYBR green.Relative occupancy is calculated using the standard curve method and fold enrichment versus IgG.Enrichment in AGI- 5198-treated cells is normalized to vehicle control.Means and standard deviation are calculated from 4 technical replicates.
Synonyms IDH-C35
Molecular Weight 462.56
Formula C27H31FN4O2
CAS No. 1355326-35-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 23 mg/mL (49.7 mM)

Ethanol: 12 mg/mL (25.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Rohle D, et al. Science, 2013, 340(6132), 626-630.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Lipid Metabolism Compound Library Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Anti-Metabolism Disease Compound Library Metabolism Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Fluorochemical Library

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Keywords

AGI-5198 1355326-35-0 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) Inhibitor inhibit AGI 5198 AGI5198 IDH-C35 inhibitor

 

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