DC Chemicals · Product datasheet

AGI-6780 — Datasheet

CAT. NO. DC7174

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ParameterValue
Chemical Name1-[5-(Cyclopropylsulfamoyl)-2-Thiophen-3-Yl-Phenyl]-3-[3-(Trifluoromethyl)phenyl]urea
CAS No.1432660-47-3
SynonymsAGI-6780;1-[5-(cyclopropylsulfamoyl)-2-thiophen-3-ylphenyl]-3-[3-(trifluoromethyl)phenyl]urea;N-Cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide;AGI 6780;FD5013;QCR-283;N-Cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide;AGI6780;AK162157;1-[5-(Cyclopropylsulfamoyl)-2-Thiophen-3-Yl-Phenyl]-3-[3-(Trifluoromethyl)phenyl]urea;MLS006011046;C21H18F3N3O3S2;AOB2268;HMS3744K17;HMS3653I21;BDBM339679;BCP07383;US10202339, Compound 124;s7241;2198AH;SB19578;NCGC0034
FormulaC21H18F3N3O3S2
M.Wt481.5111
SMILESS(C1C([H])=C([H])C(C2=C([H])SC([H])=C2[H])=C(C=1[H])N([H])C(N([H])C1=C([H])C([H])=C([H])C(C(F)(F)F)=C1[H])=O)(N([H])C1([H])C([H])([H])C1([H])[H])(=O)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2WT with IC50 of 190±8.1 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[1].

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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