性能参数

产品名称

DDP-38003 trihydrochloride

规格

10mM*1mLinDMSO1mg 5mg 10mg 50mg 100mg

货号

GOY-Y3859

 含量

>98.00%

CAS

N/A

别名

N/A

化学名

N/A

分子式

C21H29Cl3N4O

分子量

分子量 459.84

溶解度

DMSO : ≥ 120 mg/mL (260.96 mM)

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.

DDP-38003 inhibits KDM1A with an IC50 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[1].

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[1].

[1]. Vianello P, et al. Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent. J Med Chem. 2016 Feb 25;59(4):1501-17.

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