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Immunoway/AGI-6780/10mg 50mg 100mg/MC0364

    AGI-6780

    • Catalog No.:MC0364
    • Data Sheet
    • MSDS
    • Support
    • Description
    • References ( 0 )
    • Protocol
      • CasNo:
      • 1432660-47-3
      • MolecularFormula:
      • C21H18F3N3O3S
      • Purity:
      • >98%
      • Target:
      • Isocitrate Dehydrogenase (IDH)
      • IC50:
      • IC50: 23±1.7 nM (IDH2R140Q), 190±8.1 nM (IDH2WT)[1]
      • In Vitro:
      • AGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2R140Q, as well as against IDH1R132H for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1R140Q cells with AGI-6780, at concentrations that lower 2HG to near-normal physiologic levels, restore expression of both HBG and KLF1 genes and the color change associated with differentiation. AGI-6780 can reverse the IDH2R140Q-induced differentiation block in TF-1 cells. Pretreatment with AGI-6780 (0.2 μM and 1 μM) markedly decreased the intracellular concentration of (R)-2-hydroxyglutarate in the TF1R140Q cells and restored their ability to undergo EPO-induced differentiation[1].
      • In Vivo:
      • Fields:
      • AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).
      • Specificity:
      • Target:Isocitrate Dehydrogenase (IDH). Fields: AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dim
      • Source:
      • Rabbit
      • Dilution:
      • IC50: 23±1.7 nM (IDH2R140Q), 190±8.1 nM (IDH2WT)[1]
      • Concentration:
      • >98%
      • Storage Stability:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • Other Name:
      • AGI 6780; AGI6780
      • MolecularWeight(Da):
      • 481.5
      • References:
      • [1]. Wang F, et al. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science. 2013 May 3;340(6132):622-6.
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