DDP-38003 (trihydrochloride)
| 中文名称 | DDP-38003 (trihydrochloride) |
|---|---|
| 中文同义词 | KDM1A/LSD1抑制剂(DDP-38003 TRIHYDROCHLORIDE);化合物 DDP-38003 TRIHYDROCHLORIDE;化合物 T10983 |
| 英文名称 | DDP-38003 (trihydrochloride) |
| 英文同义词 | DDP-38003 (trihydrochloride) |
| CAS号 | |
| 分子式 | C??H??Cl?N?O |
| 分子量 | 0 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | Mol File |
| 结构式 |
DDP-38003 (trihydrochloride) 性质
| 形态 | 固体 |
|---|---|
| 颜色 | 黄至红褐色 |
DDP-38003 trihydrochloride是新颖，有口服活性的 KDM1A/LSD1 抑制剂，IC50值为84 nM。
IC50: 84 nM (KDM1A/LSD1)
DDP-38003 inhibits KDM1A with an IC 50 of 84 nM. DDP-38003 is more active in reducing the colony forming ability and in inducing thedifferentiation of THP-1 cells compared to the 1R, 2S analogue.
DDP-38003 exhibits in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia models with evidence of KDM1A inhibition. The half life of DDP-38003 is 8 h. A significant dose dependent increase of mice survival is obtained by DDP-38003 treatment. The survival rate increases 35% and 62% at the dose of 11.25 and 22.50 mg/kg, respectively. DDP-38003 is a potential oral anticancer agent.