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| Product Name: | EED226 | | Synonyms: | EED226;N-(furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine;MAK683(EED226/Compound 43);CS-2549;EED226;EED 226;EED226;EED 226;MAK683;1,2,4-Triazolo[4,3-c]pyrimidin-5-amine, N-(2-furanylmethyl)-8-[4-(methylsulfonyl)phenyl]-;N-[(furan-2-yl)methyl]-8-(4-methanesulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine | | CAS: | 2083627-02-3 | | MF: | C17H15N5O3S | | MW: | 369.4 | | EINECS: | | | Product Categories: | | | Mol File: | 2083627-02-3.mol |  |
| | EED226 Chemical Properties |
| density | 1.49±0.1 g/cm3(Predicted) | | storage temp. | -20° | | solubility | Soluble in DMSO (up to 25 mg/ml). | | pka | 1.19±0.30(Predicted) | | form | solid | | 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. |
| | EED226 Usage And Synthesis |
| 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).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 |
| | EED226 Preparation Products And Raw materials |
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