2083627-02-3 Usage
Description
EED226, also known as EED-226, is a potent, selective, and orally bioavailable inhibitor of the EED subunit of the methyltransferase polycomb repressive complex 2 (PRC2). It exhibits strong inhibitory effects on the growth of lymphoma cells with EZH2 mutations and has been shown to induce robust and sustained tumor regression in specific cancer models. EED226 is particularly effective as a PRC2 inhibitor in the treatment of PRC2-dependent cancers.
Uses
Used in Oncology:
EED226 is used as a potent and selective EED inhibitor for the treatment of PRC2-dependent cancers. It has demonstrated significant tumor regression in specific cancer models, making it a promising therapeutic agent for patients with these types of malignancies.
Used in Drug Development:
EED226 is used as a key compound in the development of novel cancer treatments targeting the EED subunit of PRC2. Its potent and selective inhibition of EED makes it a valuable tool for researchers and pharmaceutical companies working on developing new therapies for PRC2-dependent cancers.
Used in Preclinical Research:
EED226 is used as a research tool in preclinical studies to investigate the role of EED and PRC2 in cancer development and progression. Its ability to induce tumor regression in specific models makes it an important compound for understanding the underlying mechanisms of PRC2-dependent cancers and for identifying potential therapeutic targets.
Used in Combination Therapies:
EED226 may be used in combination with other cancer treatments to enhance the overall efficacy of therapy. Its potent inhibition of EED and PRC2-dependent cancers could potentially synergize with other targeted therapies or conventional chemotherapy, improving patient outcomes and overcoming drug resistance in certain cases.
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
Check Digit Verification of cas no
The CAS Registry Mumber 2083627-02-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 2,0,8,3,6,2 and 7 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 2083627-02:
(9*2)+(8*0)+(7*8)+(6*3)+(5*6)+(4*2)+(3*7)+(2*0)+(1*2)=153
153 % 10 = 3
So 2083627-02-3 is a valid CAS Registry Number.
2083627-02-3Relevant articles and documents
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
Huang, Ying,Zhang, Jeff,Yu, Zhengtian,Zhang, Hailong,Wang, Youzhen,Lingel, Andreas,Qi, Wei,Gu, Justin,Zhao, Kehao,Shultz, Michael D.,Wang, Long,Fu, Xingnian,Sun, Yongfeng,Zhang, Qiong,Jiang, Xiangqing,Zhang, Jiangwei,Zhang, Chunye,Li, Ling,Zeng, Jue,Feng, Lijian,Zhang, Chao,Liu, Yueqin,Zhang, Man,Zhang, Lijun,Zhao, Mengxi,Gao, Zhenting,Liu, Xianghui,Fang, Douglas,Guo, Haibing,Mi, Yuan,Gabriel, Tobias,Dillon, Michael P.,Atadja, Peter,Oyang, Counde
, p. 2215 - 2226 (2017/04/03)
Overexpression and somatic heterozygous mutations of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2), are associated with several tumor types. EZH2 inhibitor, EPZ-6438 (tazemetostat), demonstrated clinical efficacy in patients with acceptable safety profile as monotherapy. EED, another subunit of PRC2 complex, is essential for its histone methyltransferase activity through direct binding to trimethylated lysine 27 on histone 3 (H3K27Me3). Herein we disclose the discovery of a first-in-class potent, selective, and orally bioavailable EED inhibitor compound 43 (EED226). Guided by X-ray crystallography, compound 43 was discovered by fragmentation and regrowth of compound 7, a PRC2 HTS hit that directly binds EED. The ensuing scaffold hopping followed by multiparameter optimization led to the discovery of 43. Compound 43 induces robust and sustained tumor regression in EZH2MUT preclinical DLBCL model. For the first time we demonstrate that specific and direct inhibition of EED can be effective as an anticancer strategy.
