|N-[(1,2-二氢-6-甲基-2-氧代-4-丙基-3-吡啶基)甲基]-1-(1-甲基乙基)-6-[6-(4-甲基-1-哌嗪基)-3-吡啶基]-1H-吡唑并[3,4-b]吡啶-4-甲酰胺|CsnPharm

CAS No.: 1913252-04-6

JQEZ5 Catalog No. CSN22869

Synonyms: JQ-EZ-05

JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 of 11 nM.

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400-920-2911

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技术信息

生物活性

描述As a master regulator of chromatin function, the lysine methyltransferase EZH2 (enhancer of zeste homologue 2) orchestrates transcriptional silencing of developmental gene networks. Overexpression of EZH2 is commonly observed in human epithelial cancers, such as non-small cell lung carcinoma (NSCLC). JQEZ5 is a novel and potent EZH2 inhibitor which shows antitumor efficacy. Human oncogene wild-type NSCLC cells H661 treated with increasing concentrations of JQEZ5 demonstrated acutely reduced levels of H3K27me3, which prompted silencing of tumor suppressors and developmental regulators and was associated with over-expression of EZH2. This assay supported the notion that JQEZ5 was effectively targeting EZH2 in human lung cancer cell lines. Tumor-bearing mice treated with JQEZ5 for three weeks (75 mg/kg intraperitoneal (IP) daily) exhibited rapid and pronounced tumor regression over the three week treatment course. Additionally, H3K27me3 levels were largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice ^[1].
作用机制D-pyridinone ring of JQEZ5 binds to Asn78 on EZH2, and that the pyrazolo-pyridine ring is deeply buried in the S-adenosyl methionine (SAM)-binding pocket of EZH2 .
参考文献

[1] Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID: 27312177; PMCID: PMC5010480.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8427 mL
- 9.2136 mL
- 18.4272 mL
- 5 mM
- 0.3685 mL
- 1.8427 mL
- 3.6854 mL
- 10 mM
- 0.1843 mL
- 0.9214 mL
- 1.8427 mL

技术信息

CAS号

1913252-04-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H38N8O2

运输

蓝冰

分子量

542.68

别名

JQ-EZ-05

溶解度

DMSO	25.0 mg/mL (46.1 mM) warming
Water	Insoluble

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