AGI-6780
SIGMA/SML0895 - ≥98% (HPLC)
Synonym: N-
CAS Number: 1432660-47-3
Empirical Formula (Hill Notation): C21H18F3N3O3S2
Molecular Weight: 481.51
Linear Formula: C21H18F3N3O3S2
Product Type: Chemical
assay | ≥98% (HPLC) |
color | white to light brown |
form | powder |
InChI | 1S/C21H18F3N3O3S2/c22-21( |
InChI key | CCAWRGNYALGPQH-UHFFFAOYSA |
Quality Level | 100 |
solubility | DMSO: 20 mg/mL, clear |
storage temp. | 2-8°C |
Biochem/physiol Actions: | AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes. |
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Packaging: | 5, 25 mg in glass bottle |
RIDADR | NONH for all modes of transport |
WGK Germany | WGK 3 |
Flash Point(F) | Not applicable |
Flash Point(C) | Not applicable |
Purity | ≥98% (HPLC) |
Storage Temp. | 2-8°C |
UNSPSC | 12352200 |