| Molecular Formula | C27H33F3N4O3 |
| Molar Mass | 518.57 |
| Density | 1.31±0.1 g/cm3(Predicted) |
| Boling Point | 692.5±55.0 °C(Predicted) |
| Solubility | DMSO |
| pKa | 11.01±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | Treatment with EZH2 inhibitor CPI-1205 can lead to apoptosis in multiple myeloma and plasmacytoma cell models. |
| In vivo study | In in vivo experiments, CPI-1205 has excellent oral bioavailability. The animals tolerated CPI-1205 well over the course of repeated dosing without significant weight loss. In rats and dogs, CPI-1205 had relatively high blood clearance (Rat -3.19 L/h/kg, dog -1.41 L/h/kg). In both species, there is a relatively good oral availability, 44.6% and 46.2% respectively. In the toxicity test, it is well tolerated, during the recovery period, the toxic effect is reversible. |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.928 ml | 9.642 ml | 19.284 ml |
| 5 mM | 0.386 ml | 1.928 ml | 3.857 ml |
| 10 mM | 0.193 ml | 0.964 ml | 1.928 ml |
| 5 mM | 0.039 ml | 0.193 ml | 0.386 ml |
| biological activity | Lirametostat (CPI-1205) is an inhibitor of selective histone lysine methyltransferase EZH2 with oral biological activity. The IC50 for EZH2 and EZH1 is 2 nM and 52 nM respectively. It has potential anti-tumor activity. |
| target | TargetValue EZH2 (Cell-Free Assay) 2 nM EZH1 (Cell-Free Assay) 52 nM |
| Target | Value |
| EZH2 (Cell-free assay) | 2 nM |
| EZH1 (Cell-free assay) | 52 nM |
| in vitro study | in multiple myeloma and plasmacytoma cell models, the treatment of EZH2 inhibitor CPI-1205 can lead to apoptosis. |
| in vivo research | in vivo experiments, CPI-1205 have excellent oral bioavailability. In the course of repeated administration, the animals had good tolerance to CPI-1205 without significant weight loss. In rats and dogs, CPI-1205 have relatively high blood clearance rates (rats -3.19 L/h/kg, dogs -1.41 L/h/kg). In these two species, there are relatively good oral utilization, 44.6% and 46.2% respectively. In the toxicity test, it is well tolerated, and during the recovery period, the toxic effect is reversible. |