product name AGI-6780
Description: AGI-6780 is a highly potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. AGI-6780 inhibits the tumor-associated mutant IDH2/R140Q. Treatment with AGI-6780 induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. Inhibitors targeting mutant IDH2/R140Q could have potential applications as a differentiation therapy for cancer.
References: Science. 2013 May 3;340(6132):622-6.
481.51
Formula
C21H18F3N3O3S2
CAS No.
1432660-47-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 96 mg/mL (199.4 mM)
Water: <1 mg/mL
Ethanol: 96 mg/mL (199.4 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410192
| In Vitro |
In vitro activity: AGI-6780 potently reduce (R)-2-hydroxyglutarate (2HG) levels in cell lines ectopically overexpressing IDH2/R140Q with EC50 of 20 nM, with excellent selectivity against other dehydrogenases. AGI-6780 reverses the IDH2/R140Q-induced differentiation block in TF-1 cells, and induces blast differentiation in primary human IDH2/R140Q AML patient samples. Kinase Assay: Cell Assay: 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. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Science. 2013 May 3;340(6132):622-6. |
