1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide EPZ 005687
1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide.
CAS: 1396772-26-1
Molecular Formula: C32H37N5O3
1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide EPZ 005687 - Names and Identifiers
1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide EPZ 005687 - Physico-chemical Properties
| Molecular Formula | C32H37N5O3 |
| Molar Mass | 539.67 |
| Density | 1.31±0.1 g/cm3(Predicted) |
| Boling Point | 797.9±60.0 °C(Predicted) |
| Solubility | DMSO : 5 mg/mL (ultrasonic and warming) mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration chang |
| pKa | 11.88±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against the closely related enzyme EZH1. The compound reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells. |
| Target | EZH2 |
| In vitro study | EPZ005687 inhibited PRC2 enzyme activity in a concentration-dependent manner with an IC50 of 54 nM. EPZ005687 directly inhibits PRC2 enzyme activity and does not function by disrupting protein-protein interactions between PRC2 subunits. EPZ005687 binds to the SAM pocket of the EZH2 SET domain and is a SAM-competitive inhibitor of EZH2 enzyme activity. The affinity of EPZ005687 for the PRC2 complex containing wild-type and Tyr641 mutant EZH2 was similar (within a 2-fold range), the enzyme acting on the A677G mutant had a significantly higher affinity (5.4-fold). EPZ005687 acts on a variety of different lymphoma cells to reduce H3K27 methylation. It has strong lethality to heterozygous Tyr641 or Ala677 mutant cells, and has the lowest effect on the proliferation of wild-type cells. EPZ005687 increased the G1 phase of the cell cycle and, correspondingly, decreased the S and G2/M phases. EPZ005687 acts on the lymphoma cell line with Tyr641 mutation, depresses the known EZH2 target gene, and affects the gene specifically inhibited by EZH2 Tyr641 mutation. |
1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide EPZ 005687 - Reference
| Reference Show more | 1. Knutson SK, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012;8(11):890-6.2. Tang SH, et al. Effects of H3K27 methylation inhibitor EPZ005687 on apoptosis, proliferation and cell cycle of U937 cells and normal CD34 positive cells. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Dec;22(6):1561-6. |
1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide EPZ 005687 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.853 ml | 9.265 ml | 18.53 ml |
| 5 mM | 0.371 ml | 1.853 ml | 3.706 ml |
| 10 mM | 0.185 ml | 0.926 ml | 1.853 ml |
| 5 mM | 0.037 ml | 0.185 ml | 0.371 ml |
Last Update：2024-01-02 23:10:35
1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide EPZ 005687 - Cell Experiment
Plating densities are determined for each cell line on the basis of linear log-phase growth. Cells are counted and split back to the original plating density in fresh medium with EPZ005687 on days 4 and 7.(Only for Reference) Cell lines: OCI-LY19, WSU-DLCL2, Pfeiffer
Last Update：2023-08-16 21:32:38
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Spot supply
Product Name: 1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide. Visit Supplier Webpage Request for quotationCAS: 1396772-26-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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