DDP-38003 dihydrochloride |
| رقم الكتالوجGC33013 |
ثنائي هيدروكلوريد DDP-38003 هو مثبط جديد ومتوفر عن طريق الفم لمزيل ميثيلاز 1A الخاص بالهيستون ليسين (KDM1A / LSD1) مع IC 50 من 84 نانومتر
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Cas No.: 1831167-98-6
Sample solution is provided at 25 µL, 10mM.
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DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
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].
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].
[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.
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