ChemicalBook > CAS DataBase List > EED226

EED226

Product Name: EED226
CAS No.: 2083627-02-3
Chemical Name: EED226
Synonyms: EED226;CS-2549;EED226 ，S8496;EED226;EED 226;EED 226 monohydrate;EED226;EED 226;MAK683;EED226, 10 mM in DMSO;MAK683(EED226/Compound 43);1,2,4-Triazolo[4,3-c]pyrimidin-5-amine, N-(2-furanylmethyl)-8-[4-(methylsulfonyl)phenyl]-;N-(furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
CBNumber: CB93164715
Molecular Formula: C17H15N5O3S
Formula Weight: 369.4
MOL File: 2083627-02-3.mol

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EED226 Property

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.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H320Causes eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 22031
Product name: EED226
Purity: ≥99%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 22031
Product name: EED226
Purity: ≥99%
Packaging: 5mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 22031
Product name: EED226
Purity: ≥99%
Packaging: 10mg
Price: $283
Updated: 2024/03/01

Cayman Chemical

Product number: 22031
Product name: EED226
Purity: ≥99%
Packaging: 25mg
Price: $573
Updated: 2024/03/01

TRC

Product number: E338000
Product name: EED226
Packaging: 5mg
Price: $275
Updated: 2021/12/16

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EED226 Chemical Properties,Usage,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 EZH2^MUT 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 t_1/2 (2.2 h), and moderate plasma protein binding (PPB)^[2].

storage

Store at -20°C

References

[1] YING HUANG*. Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy[J]. Journal of Medicinal Chemistry, 2017, 60 6: 2215-2226. DOI:10.1021/acs.jmedchem.6b01576
[2] WEI QI. An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED[J]. Nature chemical biology, 2017, 13 4: 381-388. DOI:10.1038/nchembio.2304

EED226 Preparation Products And Raw materials

Raw materials

Preparation Products

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EED226 Suppliers

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2083627-02-3, EED226Related Search:

AG 490 Brefeldin A Ko 143 ZM 336372

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

EED226, 10 mM in DMSO

EED 226 monohydrate

EED226 ，S8496

2083627-02-3