[CAS NO. 1432660-47-3] AGI-6780
PRODUCTS SPECIFICATIONS [1432660-47-3]
DESCRIPTION [1432660-47-3]
Overview
| MDL | MFCD26097285 |
|---|---|
| Molecular Weight | 481.51 |
| Molecular Formula | C21H18F3N3O3S2 |
| SMILES | O=S(C1=CC=C(C2=CSC=C2)C(NC(NC3=CC=CC(C(F)(F)F)=C3)=O)=C1)(NC4CC4)=O |
6 Publications Citing Use of MCE
Summary
AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2 R140Q with IC 50 of 23±1.7 nM. AGI-6780 is less potent against IDH2 WT with IC 50 of 190±8.1 nM.
IC50 & Target
IC50: 23±1.7 nM (IDH2 R140Q ), 190±8.1 nM (IDH2 WT ) [1]
In Vitro
AGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2 R140Q , as well as against IDH1 R132H for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1 R140Q 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 IDH2 R140Q -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 TF1 R140Q cells and restored their ability to undergo EPO-induced differentiation [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 29 mg/mL ( 60.23 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0768 mL | 10.3840 mL | 20.7680 mL |
| 5 mM | 0.4154 mL | 2.0768 mL | 4.1536 mL |
| 10 mM | 0.2077 mL | 1.0384 mL | 2.0768 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution