DDP-38003 dihydrochloride 是具有口服活性的KDM1A/LSD1抑制剂,IC50 值为 84 nM。
产品描述
DDP-38003 dihydrochloride is an orally available histone lysine-specific demethylase 1A (KDM1A/LSD1) inhibitor (IC50: 84 nM).
体外活性
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 inhibits KDM1A (IC50: 84 nM) [1].
体内活性
DDP-38003 is a potential oral anticancer agent. The half life of DDP-38003 is 8 h. DDP-38003 shows in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia models with evidence of KDM1A inhibition. 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[1].
Cas No.
1831167-98-6
分子式
C21H28Cl2N4O
分子量
423.38
储存和溶解度
DMSO:27mg/mL (63.8mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years