AGI-6780
AGI-6780 is a potent and selective inhibitor of tumor-associated IDH2/R140Q mutation with IC50 value of 23 nM [1].
AGI-6780 could significantly reduce intracellular concentration of 2HG in the human glioblastoma TF1/R140Q cells, as well as reverse IDH2/R140Q-mediated differentiation block in TF1 cells in the presence of EPO. AGI-6780 could restore KLF1 and hemoglobin G1/2 expressions in the EPO-induced TF1/R140Q cells [1].
References:
[1] Wang F1, Travins J, DeLaBarre B, Penard-Lacronique V, Schalm S, Hansen E, Straley K, Kernytsky A, Liu W, Gliser C, Yang H, Gross S, Artin E, Saada V,Mylonas E, Quivoron C, Popovici-Muller J, Saunders JO, Salituro FG, Yan S, Murray S, Wei W, Gao Y, Dang L, Dorsch M, Agresta S, Schenkein DP, Biller SA, Su SM, de Botton S, Yen KE. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science. 2013 May 3;340(6132):622-6.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 481.51 |
| Cas No. | 1432660-47-3 |
| Formula | C21H18F3N3O3S2 |
| Synonyms | AGI 6780;AGI6780 |
| Solubility | ≥22.25 mg/mL in DMSO; insoluble in H2O; ≥100.8 mg/mL in EtOH |
| Chemical Name | 1-[5-(cyclopropylsulfamoyl)-2-thiophen-3-ylphenyl]-3-[3-(trifluoromethyl)phenyl]urea |
| SDF | Download SDF |
| Canonical SMILES | C1CC1NS(=O)(=O)C2=CC(=C(C=C2)C3=CSC=C3)NC(=O)NC4=CC=CC(=C4)C(F)(F)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Primary human AML cells |
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Preparation method |
The solubility of this compound in DMSO is > 22.25 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
5 μM up to 10 days |
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Applications |
IDH2 mutant samples treated with AGI-6780 showed a dose-dependent reduction in the amounts of extracellular and intracellular (R)-2-hydroxyglutarate. In the presence AGI-6780, a burst of cell proliferation was also observed only in the IDH2/R140Q mutant samples. Furthermore, AGI-6780 did not exert a cytotoxic effect as the number of viable, more mature CD45-positive cells increased in the presence of AGI-6780 only in the IDH2/R140Q mutant samples whereas the IDH2/WT samples remained unchanged. |
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References: [1] Wang F1,Travins J,DeLaBarre B,Penard-Lacronique V,Schalm S,Hansen E,Straley K,Kernytsky A,Liu W,Gliser C,Yang H,Gross S,Artin E,Saada V,Mylonas E,Quivoron C,Popovici-Muller J,Saunders JO,Salituro FG,Yan S,Murray S,Wei W,Gao Y,Dang L,Dorsch M,Agresta S,Schenkein DP,Biller SA,Su SM,de Botton S,Yen KE. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science.2013 May 3;340(6132):622-6. |
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| Description | AGI-6780 is a potent and time-dependent inhibitor of IDH2-R140Q with IC50 values of 23±1.7 nM and 190±8.1 nM for IDH2-R140Q and IDH2-WT,respectively. | |||||
| Targets | IDH2-R140Q | IDH2-WT | ||||
| IC50 | 23±1.7 nM | 190±8.1 nM | ||||
Quality Control & MSDS
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Chemical structure
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