EED226|2083627-02-3--Shanghai xingMo Biotechnology

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Description

EED226 is a potent, selective, and orally bioavailable EED inhibitor. induces robust and sustained tumor regression in EZH2MUT preclinical DLBCL model. EED226 induces a conformational change upon binding EED, leading to loss of PRC2 activity. EED226 shows similar activity to SAM-competitive inhibitors in blocking H3K27 methylation of PRC2 target genes and inducing regression of human lymphoma xenograft tumors. Interestingly, EED226 also effectively inhibits PRC2 containing a mutant EZH2 protein resistant to SAM-competitive inhibitors. EED226 inhibits PRC2 activity via an allosteric mechanism and offers an opportunity for treatment of PRC2-dependent cancers. demonstrated very impressive antitumor activities in mouse xenograft model.

Chemical Structure

Chemical Name

N-(Furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)[1,2,4]-triazolo[4,3-c]pyrimidin-5-amine

SMILES Code

O=S(C1=CC=C(C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)C=C1)(C)=O

Theoretical Analysis

XingMo Cat#:XM480
Product Name:EED226
Synonyms:EED226; EED-226; EED 226.
CAS#:2083627-02-3
Chemical Formula:C₁₇H₁₅N₅O₃S
Exact Mass:369.0896
Molecular Weight:369.399

Technical Data

Appearance: Solid powder

Purity:>98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years)

Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 - 4 ℃ for short term (days to weeks), or -20 ℃ for long term (months).

WARNING: This product is for research use only, not for human or veterinary use

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