| CAS NO: | 1831167-98-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 423.38 |
|---|---|
| Formula | C21H28Cl2N4O |
| CAS No. | 1831167-98-6 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 29 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: | |
| SMILES | O=C(NC1=CC=C([C@H]2[C@H](N)C2)C=C1)C3=CC=C(N4CCN(C)CC4)C=C3.[H]Cl.[H]Cl |
| Synonyms | DDP-38003 dihydrochloride; DDP 38003 dihydrochloride; DDP38003 dihydrochloride; DDP-38003 2HCl; DDP 38003 2HCl; DDP38003 2HCl |
| In Vitro | In vitro activity: DDP-38003 dihydrochloride, a tranylcypromine (TCPA) derivative, is an novel, orally bioavailable inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1). 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. It exhibited in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia model with evidence of KDM1A inhibition. The biological profile of DDP-38003 supports its further investigation as a cancer therapeutic. Kinase Assay: DDP-38003 inhibits KDM1A with an IC50 of 84 nM. Cell Assay: 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 |
|---|---|
| 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 |
| Animal model | Mouse leukemia models |
| Formulation & Dosage | Dissolved in 40% PEG 400 in a 5% glucose solution; 11.25 and 22.50 mg/kg; oral admin. |
| References | J Med Chem. 2016 Feb 25;59(4):1501-17. |
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