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AGI-6780

Catalog No. T1809   CAS 1432660-47-3

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
AGI-6780 Chemical Structure
AGI-6780, CAS 1432660-47-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 122.00
25 mg In stock $ 232.00
50 mg In stock $ 413.00
100 mg In stock $ 618.00
500 mg In stock $ 1,330.00
1 mL * 10 mM (in DMSO) In stock $ 77.00
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Purity: 98.15%
Purity: 97.47%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.
Targets&IC50 IDH2 R140Q mutant:23 nM
Kinase Assay AGI-6780 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-ketoglutarate 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 Em590[1].
Cell Research AGI-6780 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. Cells are sorted from fresh or frozen bone marrow aspirates and blood samples after labelling with PE-CD34, APC-CD38, PE-CD14, FITC-CD3 (clone HIT3a) and PECy7-CD19 (clone SJ25C1) antibodies using a MoFlow cell sorter. Unfractionated nucleated blood or bone marrow cells are plated in Methocult H4434 methylcellulose medium at 104 cells/dish, in duplicate dishes per condition. AGI-6780 (5 mM) is directly added to the medium. Dishes are incubated in a humidified incubator at 37°C and colonies containing at least 30 cells are counted after 13 days[1].
Molecular Weight 481.51
Formula C21H18F3N3O3S2
CAS No. 1432660-47-3

Storage

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

Solubility Information

DMSO: 89 mg/mL (184.8 mM)

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

Ethanol: 89 mg/mL (184.8 mM)

TargetMolReferences and Literature

1. Wang F, et al. Science. 2013, 340(6132), 622-666. 2. Chen J, Yang J, Wei Q, et al. Cell Communication and Signaling. 2020, 18(1): 1-12. 3. Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells[J]. Cell Communication and Signaling. 2020, 18: 1-12. 4. Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells[J]. Cell Communication and Signaling . 2020, 18: 1-12.

TargetMolCitations

1. Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells. Cell Communication and Signaling. 2020, 18(1): 1-12 2. Tan Q, Zhang X, Li S, et al.DMT1 differentially regulates mitochondrial complex activities to reduce glutathione loss and mitigate ferroptosis.Free Radical Biology and Medicine.2023 3. Yang J, Chen J, Chang J, et al.IDH2/R140Q mutation confers cytokine-independent proliferation of TF-1 cells by activating constitutive STAT3/5 phosphorylation.Cell Communication and Signaling.2024, 22(1): 116.

Related compound libraries

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

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MF-438 KPLH1130 JX06 Ethionamide AGI-14100 IDH2R140Q-IN-2 ALDH2 modulator 1 Epostane

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Keywords

AGI-6780 1432660-47-3 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) inhibit AGI6780 Inhibitor AGI 6780 inhibitor

 

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