AGI-6780
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. (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.
Product Specifications
CAS Number
1432660-47-3
Product Name Alternative
AGI6780 | AGI 6780 | AGI-6780
Purity
>98% (HPLC)
Solubility
Ethanol: 96 mg/mL (199.37 mM) ; DMSO: 96 mg/mL (199.37 mM)
Smiles
O=S (C1=CC=C (C2=CSC=C2) C (NC (NC3=CC=CC (C (F) (F) F) =C3) =O) =C1) (NC4CC4) =O
Molecular Formula
C21H18F3N3O3S2
Molecular Weight
481.51
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
N-cyclopropyl-4- (thiophen-3-yl) -3- (3- (3- (trifluoromethyl) phenyl) ureido) benzenesulfonamide
Available Sizes
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