EED226
- CAS No.
- 2083627-02-3
- Chemical Name:
- EED226
- Synonyms
- EED226;CS-2549;EED226;EED 226;EED 226 monohydrate;EED226, 10 mM in DMSO;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]-;N-[(furan-2-yl)methyl]-8-(4-methanesulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
- CBNumber:
- CB93164715
- Molecular Formula:
- C17H15N5O3S
- Molecular Weight:
- 369.4
- MDL Number:
- MFCD30738018
- MOL File:
- 2083627-02-3.mol
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H320-H335 | |||||||||
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 | |||||||||
| NFPA 704 |
|
EED226 price More Price(21)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 22031 | EED226 ≥99% | 2083627-02-3 | 1mg | $37 | 2024-03-01 | Buy |
| Cayman Chemical | 22031 | EED226 ≥99% | 2083627-02-3 | 5mg | $161 | 2024-03-01 | Buy |
| Cayman Chemical | 22031 | EED226 ≥99% | 2083627-02-3 | 10mg | $283 | 2024-03-01 | Buy |
| Cayman Chemical | 22031 | EED226 ≥99% | 2083627-02-3 | 25mg | $573 | 2024-03-01 | Buy |
| TRC | E338000 | EED226 | 2083627-02-3 | 5mg | $275 | 2021-12-16 | Buy |
EED226 Chemical Properties,Uses,Production
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.
in vivo
EED226 induces robust and sustained tumor regression in EZH2MUT pre-clinical DLBCL model. In CD-1 mice, dosing of EED226 for 14 days at 300 mg/kg bid is well tolerated with no apparent adverse effects. It has very low in vivo clearance, and approximately 100% oral bioavailability. EED226 has low volume of distribution (0.8 L/kg), reasonable terminal t1/2 (2.2 h), and moderate plasma protein binding (PPB)[2].
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
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30230 | 58 |
| Labnetwork lnc. | +86-27-50766799 +8618062016861 | contact@labnetwork.com | China | 19987 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38630 | 58 | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43340 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 |
| Supplier | Advantage |
|---|---|
| ATK CHEMICAL COMPANY LIMITED | 60 |
| BOC Sciences | 58 |
| TargetMol Chemicals Inc. | 58 |
| Career Henan Chemica Co | 58 |
| Labnetwork lnc. | 58 |
| InvivoChem | 58 |
| TargetMol Chemicals Inc. | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 58 |
| LEAPCHEM CO., LTD. | 58 |
| Aladdin Scientific | 58 |
