DACA

DACA (XR 5000) is a potential and blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer^[1][2][3][4]. In Vitro:DACA (0.1-100 μM; 2 h) stabilizes topoisomerase II cleavable complexes in a dose-dependent manner in human leukaemia CCRF-CEM cells, forms topoisomerase IIβ cleavable complexes only at the highest concentration of 100 μM^[1].
DACA exhibits a pattern of activity distinct from that of Amsacrine (HY-13551) and Etoposide (HY-13629) against a variety of human and mouse cell lines, including primary human melanoma cultures derived from fresh surgical melanoma specimens, with IC₅₀ values ranging from 0.09 μM to 3.4 μM^[4].
In Vivo:DACA is highly active against Lewis lung carcinoma in mice^[4].
Studies have shown that DACA has significant potential for clinical application. First, DACA can overcome drug resistance in various types of cancer cells. Second, DACA exhibits high activity against certain solid tumor models in vitro and in vivo. Third, DACA appears to be able to cross the blood-brain barrier in animal models. Finally, DACA exhibits linear pharmacokinetic characteristics in preclinical models^[5].