DDP-38003-trihydrochloride - Histone Demethylase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDDP-38003 trihydrochlorideCat. No.: HY-19612B分式: CHClNO分量: 459.84作靶點(diǎn): Histone Demethylase作通路: Epigenetics儲(chǔ)存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 120 mg/mL

2、 (260.96 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.1747 mL 10.8733 mL 21.7467 mL5 mM 0.4349 mL 2.1747 mL 4.3493 mL10 mM 0.2175 mL 1.0873 mL 2.1747 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 DDP-38003 trihydrochloride新穎，有

3、服活性的 KDM1A/LSD1 抑制劑，IC50值為84 nM。IC50 & Target IC50: 84 nM (KDM1A/LSD1) 1體外研究 DDP-38003 inhibits KDM1A with an IC50 of 84 nM. DDP-38003 is more active in reducing the colony formingability and in inducing thedifferentiation of THP-1 cells compared to the 1R, 2S analogue 1.體內(nèi)研究DDP-38003 exhibits in vi

4、vo efficacy after oral administration, determining a 62% increased survival in mouseleukemia models with evidence of KDM1A inhibition. The half life of DDP-38003 is 8 h. A significant dose1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEdependent increase of mice survival is obtained by DDP-38003 tr

5、eatment. 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 agent1.PROTOCOLAnimal Mice: CD-1 mice is used in the study. DDP-38003 is dissolved (40% PEG 400 in a 5% glucose solution) andAdministration 1 orally administer

6、ed 3 days per week (Monday, Tuesday and Wednesday) for 3 weeks at the doses of 11.25mg/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 andrep

7、resented by a Kaplan-Meier survival plot 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Vianello P, et al. Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active AntitumorAgent. J Med Chem. 2016 Feb 25;59(4):1501-17.McePdfHeightCaution: Product has not been fully validated for medical applications.For research