1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-
CPI-360
CAS: 1802175-06-9
Molecular Formula: C25H31N3O4
1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]- - Names and Identifiers
1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]- - Physico-chemical Properties
| Molecular Formula | C25H31N3O4 |
| Molar Mass | 437.53 |
| Density | 1.26±0.1 g/cm3(Predicted) |
| Boling Point | 712.2±60.0 °C(Predicted) |
| Solubility | DMSO: ≥ 48.9 mg/mL |
| pKa | 11.01±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | In KARPAS-422 cells, CPI-360 effectively reduced overall H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also caused alterations in time-dependent transcription and affected the activity of the Y641N mutant in KARPAS-422 cells containing EZH2. In addition, CPI-360 gradually blocks KARPAS-422 cells at the G1 cell cycle stage and subsequently induces apoptosis. |
| In vivo study | In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduced tumor growth by 44%. |
1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.286 ml | 11.428 ml | 22.856 ml |
| 5 mM | 0.457 ml | 2.286 ml | 4.571 ml |
| 10 mM | 0.229 ml | 1.143 ml | 2.286 ml |
| 5 mM | 0.046 ml | 0.229 ml | 0.457 ml |
Last Update：2024-01-02 23:10:35
1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]- - Reference Information
| biological activity | CPI-360 is a potent, selective, and SAM competitive EZH1 inhibitor with an IC50 of 102.3 nM, the selectivity is more than 100-fold higher than for other methyltransferases. |
| Target | Value |
| EZH1 () | 102.3 nM |
Last Update：2024-04-09 21:21:28
![1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-](http://res.chembk.com/assets/str/2d/1/18/1802175-06-9.png)
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Product Name: CPI-360 Visit Supplier Webpage Request for quotation
CAS: 1802175-06-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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CAS: 1802175-06-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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