AGI-6780

SKU: orb1307400

Description

AGI-6780

Research Area

Metabolism Research

Key Properties

• CAS Number: 1432660-47-3
• MW: 481.51
• Purity: 99.70%
• Formula: C₂₁H₁₈F₃N₃O₃S₂
• SMILES: FC(F)(F)c1cccc(NC(=O)Nc2cc(ccc2-c2ccsc2)S(=O)(=O)NC2CC2)c1
• Target: Isocitrate Dehydrogenase (IDH),Dehydrogenase
• Solubility: DMSO:125 mg/mL (259.6 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.85 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:89 mg/mL (184.84 mM)

Bioactivity

• Target IC50:
  IDH2 (R140Q):23 nM
• In Vivo:
  AGI-6780 reverses differentiation blockage induced by IDH2/R140Q in TF-1 cells and induces rapid differentiation in primary samples from patients with IDH2/R140Q AML. It effectively reduces the levels of (R)-2-hydroxyglutarate (2-HG) in cell lines overexpressing ectopic IDH2/R140Q, with an EC50 of 20 nM, demonstrating excellent selectivity compared to other dehydrogenases.
• Cell Research:
  AGI-6780 is dissolved in DMSO and stored, and then diluted with appropriate media before use. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AGI6780, AGI-6780, AGI 6780, IDH2 R140Q mutant, IDH, Inhibitor, IsocitrateDehydrogenase(IDH), Isocitrate Dehydrogenase, Isocitrate Dehydrogenase (IDH), IsocitrateDehydrogenase, inhibit

Compound Identifiers

PubChem CID

71299339