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Enasidenib

Chemical Structure : Enasidenib

CAS No.: 1446502-11-9

Enasidenib (AG-221, CC-90007, AG221)

Catalog No.: PC-45529Not For Human Use, Lab Use Only.

Enasidenib (AG-221, CC-90007) is an orally available, selective, potent inhibitor of mutant IDH2 with IC50s of 100-400 nM for IDH2R140Q homodimer, IDH2R172K homodimer and IDH2WT/R140Q, IDH2WT/R172K.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Enasidenib (AG-221, CC-90007) is an orally available, selective, potent inhibitor of mutant IDH2 with IC50s of 100-400 nM for IDH2R140Q homodimer, IDH2R172K homodimer and IDH2WT/R140Q, IDH2WT/R172K.
Enasidenib (AG-221, CC-90007) is less potent for IDH2WT homodimer and IDH1WT homodimer.
Enasidenib (AG-221, CC-90007) suppresses 2HG production and induces cellular differentiation in primary human IDH2 mutation-positive AML cells ex vivo and in xenograft mouse models.

Physicochemical Properties

M.Wt 473.375
Formula C19H17F6N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Propanol, 2-methyl-1-[[4-[6-(trifluoromethyl)-2-pyridinyl]-6-[[2-(trifluoromethyl)-4-pyridinyl]amino]-1,3,5-triazin-2-yl]amino]-

References

1. Yen K, et al. Cancer Discov. 2017 May;7(5):478-493.

2. Kats LM, et al. Leukemia. 2017 Apr 11. doi: 10.1038/leu.2017.84.

3. Shih AH, et al. Cancer Discov. 2017 May;7(5):494-505.

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