[CAS NO. ] DDP-38003trihydrochloride

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PRODUCTS SPECIFICATIONS

Catalog

HY-19612B

Brand

MCE

CAS

-

DESCRIPTION

Overview

MDL	-
Molecular Weight	459.84
Molecular Formula	C21H29Cl3N4O
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

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

Summary

DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A ( KDM1A/LSD1 ) with an IC ₅₀ of 84 nM.

IC50 & Target

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

In Vitro

DDP-38003 inhibits KDM1A with an IC ₅₀ 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.

Appearance

Solid

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)

H ₂ O : 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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 50 mg/mL (108.73 mM); Clear solution; Need ultrasonic
2.

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
3.

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

* All of the co-solvents are available by MCE.

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.