Quinacrine hydrochloride hydrate [6151-30-0]

Quinacrine Dihydrochloride Dihydrate is an orally available antimalarial agent capable of crossing the blood-brain barrier. It exhibits anticancer activity by inhibiting WNT/TCF and topoisomerase, inducing autophagy and apoptosis, and activating p53. Quinacrine is an acridine dye derivative used for DNA and RNA staining in fixed cells (Ex/Em=436/525 nm).

Quinacrine Dihydrochloride Dihydrate inhibits the growth of SGC-7901 cells at concentrations of 5-20 μM with an exposure time of 24 hours [1].
Quinacrine Dihydrochloride Dihydrate induces apoptosis in SGC-7901 cells at concentrations of 7.5 and 15 μM with an exposure time of 24 hours; this apoptotic process is associated with the mitochondrial-dependent signaling pathway and involves upregulation of p53 protein and activation of the caspase-3 protein pathway [1].
Treatment of cells with Quinacrine Dihydrochloride Dihydrate at a concentration of 15 μM for 24 hours significantly increases the levels of pro-apoptotic proteins (including cytochrome c, Bax protein, and p53 protein) while reducing the level of the anti-apoptotic protein Bcl-2, thereby shifting the Bax/Bcl-2 ratio in a direction favorable to apoptosis [1].

Quinacrine Dihydrochloride Dihydrate (100 mg/kg, administered via gavage, three times per week for two consecutive weeks) reduced the proportion of homo sapiens-derived tumor cells in female severe combined immunodeficiency (SCID) mice with acute myeloid leukemia (AML)-PS models to 2.2%, and extended the median survival time of the mice to 46 days [2].