| Identification | Back Directory | [Name]
EED226 | [CAS]
2083627-02-3 | [Synonyms]
EED226
CS-2549
EED226;EED 226
EED226;EED 226;MAK683
MAK683(EED226/Compound 43)
N-(furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
1,2,4-Triazolo[4,3-c]pyrimidin-5-amine, N-(2-furanylmethyl)-8-[4-(methylsulfonyl)phenyl]- | [Molecular Formula]
C17H15N5O3S | [MDL Number]
MFCD30738018 | [MOL File]
2083627-02-3.mol | [Molecular Weight]
369.4 |
| Chemical Properties | Back Directory | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (up to 25 mg/ml). | [form ]
solid | [pka]
1.19±0.30(Predicted) | [color ]
Off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
EED-226 (2083627-02-3) is a potent (IC50?= 23.4 nM) ?and selective allosteric inhibitor of the EED subunit of the methyltransferase polycomb repressive complex 2 (PRC2).1,2?It caused drastic proliferation inhibition in lymphoma cells with EZH2 mutations and caused shrinkage and slower tumor growth in mice using a subcutaneous xenograft model of Karpas422. | [Uses]
EED 226 is a potent, selective and orally bioavailable EED inhibitor, inducing robust and sustained tumor regression in specific models. Effective PRC2 inhibitorin the treatment of PRC2-dependant cancers. | [storage]
Store at -20°C | [References]
1) Huang?et al.?(2017),?Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy; J. Med. Chem.?60?2215
2) Qi?et al.?(2017),?An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED; Nat. Chem. Biol.?13?381 |
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