DDP-38003 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DDP-38003 是一种新型口服组蛋白赖氨酸特异性去甲基酶 1A (KDM1A/LSD1) 抑制剂，IC50 为 84 nM。

DDP-38003 is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with IC50 of 84 nM; weakly inhibits MAO-A and has no activity for KDM1B and MAO-B (IC50>30 uM); orally bioactive and exhibits in vivo efficacy in mouse leukemia model.Blood Cancer Preclinical.

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.

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.

DDP 38003 dihydrochloride | DDP38003 dihydrochloride

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

Cancer

Blood cancer

1831167-98-6

423.37922

C21H28Cl2N4O

>98% (HPLC)

DMSO: ≥ 29 mg/mL

CN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3=CC=C(C=C3)C4CC4N.Cl.Cl

Benzamide, N-[4-[(1S,2R)-2-aminocyclopropyl]phenyl]-4-(4-methyl-1-piperazinyl)-, hydrochloride (1:2)

(-20℃)

With Ice Pack

≥ 2 years