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[CAS NO. ] DDP-38003trihydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19612B |
| Brand: | MCE |
| CAS: | - |
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 |
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
DMSO : 100 mg/mL ( 217.47 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 108.73 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (108.73 mM); Clear solution; Need ultrasonic
-
2.
-
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
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