CAS No. 2083627-02-3
| IUPAC Name | N-(furan-2-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine | |
|---|---|---|
| CAS Number | 2083627-02-3 | |
| Molecular Formula |
C17H15N5O3S |
|
| Molecular Weight (MW) | 369.40 | |
| SMILES | CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(N3C2=NN=C3)NCC4=CC=CO4 | |
| InChIKey | DYIRSNMPIZZNBK-UHFFFAOYSA-N |
EED226 is a potent, selective, and orally bioavailable allosteric Polycomb repressive complex 2 (PRC2) inhibitor that directly binds to the H3K27me3-binding pocket of EED, inhibiting PRC2 methyltransferase activity with an IC50 ofusing H3K27me0 peptide substrate and an IC50 ofusing mononucleosome substrate. By disrupting allosteric activation of PRC2, EED226 induces loss of cellular H3K27me3 levels, derepresses PRC2-target genes, and suppresses tumor growth in preclinical models. [1]
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Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
73 mg/mL
(197.61 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Water | Insoluble |
| Ethanol | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
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