1. Epigenetics
  2. Histone Demethylase
  3. DDP-38003 dihydrochloride

DDP-38003 dihydrochloride 

Cat. No.: HY-19612A
Handling Instructions

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

For research use only. We do not sell to patients.

DDP-38003 dihydrochloride Chemical Structure

DDP-38003 dihydrochloride Chemical Structure

CAS No. : 1831167-98-6

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Description

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

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

423.38

Formula

C21H28Cl2N4O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 29 mg/mL (68.50 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3619 mL 11.8097 mL 23.6194 mL
5 mM 0.4724 mL 2.3619 mL 4.7239 mL
10 mM 0.2362 mL 1.1810 mL 2.3619 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
DDP-38003 dihydrochloride
Cat. No.:
HY-19612A
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