EED226
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.
Product Specifications
CAS Number
2083627-02-3
Product Name Alternative
EED226 | EED-226 | EED 226
Purity
>98% (HPLC)
Solubility
DMSO : ≥ 29 mg/mL. 78.51 mM; H2O : < 0.1 mg/mL
Smiles
C1 (n2c (c (cn1) c1ccc (cc1) S (=O) (=O) C) nnc2) NCc1occc1
Molecular Formula
C17H15N5O3S
Molecular Weight
369.4
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
N- (Furan-2-ylmethyl) -8- (4- (methylsulfonyl) phenyl) [1,2,4]-triazolo[4,3-c]pyrimidin-5-amine
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