Molecular Formula | C21H18F3N3O3S2 |
Molar Mass | 481.51 |
Density | 1.52±0.1 g/cm3(Predicted) |
pKa | 11.78±0.20(Predicted) |
Storage Condition | -20℃ |
In vitro study | AGI-6780 can effectively reduce the ectopic overexpression of IDH2/R140Q in cell lines (R)-2-Hydroxyglutaric acid (2HG) level, EC50 is 20 nM, compared with other dehydrogenase, with excellent selectivity. AGI-6780 reverses IDH2/R140Q induced differentiation arrest in TF-1 cells and induces sharp differentiation in primary human IDH2/R140Q AML patient samples. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.077 ml | 10.384 ml | 20.768 ml |
5 mM | 0.415 ml | 2.077 ml | 4.154 ml |
10 mM | 0.208 ml | 1.038 ml | 2.077 ml |
5 mM | 0.042 ml | 0.208 ml | 0.415 ml |
biological activity | AGI-6780 is a potent selective IDH2 R140Q mutant inhibitor with an IC50 of 23 nM. |
in vitro study | AGI-6780 can effectively reduce the (R)-2-hydroxyglutaric acid (2HG) level of ectopic overexpression of IDH2/R140Q in cell lines, with EC50 of 20 nM, which has excellent selectivity compared with other dehydrogenases. AGI-6780 reversed IDH2/R140Q-induced differentiation arrest in TF-1 cells and induced sharp differentiation in primary human IDH2/R140QAML patient samples. |