DDP-38003 trihydrochloride

Cat. No.: HY-19612B: FAQs
Data Sheet SDS Handling Instructions

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DDP-38003 trihydrochloride 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 trihydrochloride Chemical Structure

Size	Price	Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 172	Ask For Quote & Lead Time
Solution
10 mM * 1 mL in DMSO	USD 172	Ask For Quote & Lead Time
Solid
1 mg	USD 90	Ask For Quote & Lead Time
5 mg	USD 170	Ask For Quote & Lead Time
10 mg	USD 290	Ask For Quote & Lead Time
50 mg	USD 1100	Ask For Quote & Lead Time
100 mg	USD 1900	Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of DDP-38003 trihydrochloride:

DDP-38003 dihydrochloride Get quote

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•Related Small Molecules:

•Related Proteins:

View All Histone Demethylase Isoform Specific Products:

View All Isoforms

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

DDP-38003 trihydrochloride 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].

MedChemExpress (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].

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

Molecular Weight

459.84

Formula

C₂₁H₂₉Cl₃N₄O

Appearance

Solid

Color

Yellow to reddish brown

SMILES

[H]Cl.[H]Cl.O=C(NC1=CC=C([C@@H]2C[C@H]2N)C=C1)C(C=C3)=CC=C3N4CCN(C)CC4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (217.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (108.73 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1747 mL	10.8733 mL	21.7467 mL
5 mM	0.4349 mL	2.1747 mL	4.3493 mL
10 mM	0.2175 mL	1.0873 mL	2.1747 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (108.73 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Data Sheet (272 KB) SDS (251 KB) Handling Instructions (2659 KB)

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. [Content Brief]

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

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.1747 mL	10.8733 mL	21.7467 mL	54.3667 mL
	5 mM	0.4349 mL	2.1747 mL	4.3493 mL	10.8733 mL
	10 mM	0.2175 mL	1.0873 mL	2.1747 mL	5.4367 mL
	15 mM	0.1450 mL	0.7249 mL	1.4498 mL	3.6244 mL
	20 mM	0.1087 mL	0.5437 mL	1.0873 mL	2.7183 mL
	25 mM	0.0870 mL	0.4349 mL	0.8699 mL	2.1747 mL
	30 mM	0.0725 mL	0.3624 mL	0.7249 mL	1.8122 mL
	40 mM	0.0544 mL	0.2718 mL	0.5437 mL	1.3592 mL
	50 mM	0.0435 mL	0.2175 mL	0.4349 mL	1.0873 mL
	60 mM	0.0362 mL	0.1812 mL	0.3624 mL	0.9061 mL
	80 mM	0.0272 mL	0.1359 mL	0.2718 mL	0.6796 mL
	100 mM	0.0217 mL	0.1087 mL	0.2175 mL	0.5437 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.