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.

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.

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.

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