CPI-360 (R) - Names and Identifiers
CPI-360 (R) - 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%. |
CPI-360 (R) - 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
CPI-360 (R) - 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