DDP-38003 dihydrochloride

Modify Date: 2024-01-08 09:27:11

DDP-38003 dihydrochloride Structure
DDP-38003 dihydrochloride structure
Common Name DDP-38003 dihydrochloride
CAS Number 1831167-98-6 Molecular Weight 423.379
Density N/A Boiling Point N/A
Molecular Formula C21H28Cl2N4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of DDP-38003 dihydrochloride


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

 Names

Name DDP-38003 dihydrochloride
Synonym More Synonyms

 DDP-38003 dihydrochloride Biological Activity

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

IC50: 84 nM (KDM1A/LSD1)[1]

In Vitro 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].
In Vivo 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].
Animal Admin Mice: CD-1 mice is used in the study. DDP-38003 is dissolved (40% PEG 400 in a 5% glucose solution) and orally administered 3 days per week (Monday, Tuesday and Wednesday) for 3 weeks at the doses of 11.25 mg/kg and 22.5 mg/kg. The treatment started once blast cells are detected in the recipients' peripheral blood (10 days after cell injection). The survival of mice of the different experimental groups is analyzed and represented by a Kaplan-Meier survival plot[1].
References

[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.

 Chemical & Physical Properties

Molecular Formula C21H28Cl2N4O
Molecular Weight 423.379
Exact Mass 422.164032
Storage condition 2-8℃

 Synonyms

Benzamide, N-[4-[(1S,2R)-2-aminocyclopropyl]phenyl]-4-(4-methyl-1-piperazinyl)-, hydrochloride (1:2)
N-{4-[(1S,2R)-2-Aminocyclopropyl]phenyl}-4-(4-methyl-1-piperazinyl)benzamide dihydrochloride
DDP-38003 (dihydrochloride)