Chloroquine phosphate (50-63-5) is an antimalarial drug. Inhibits autophagy in a variety of cell lines.1 Induces cell death in breast cancer cell lines and displays antitumor and antimetastatic activity in mouse models of breast cancer.2 Eliminates cancer stem cells via deregulation of JAK2 and DNMT1.3 Chloroquine phosphate displays synergy when combined with the Raf inhibitor, vemurafenib, in brain tumors.4 Cell permeable and active in vivo.
1) Frieboes et al. (2014), Chloroquine-mediated cell death in metastatic pancreatic adenocarcinoma through inhibition of autophagy; JOP, 15 189
2) Jiang et al. (2010), Antitumor and antimetastatic activities of chloroquine diphosphate in a murine model of breast cancer; Biomed. Pharmacother., 64 609
3) Choi et al. (2014), Chloroquine eliminates cancer stem cells through deregulation of Jak2 and DNMT1; Stem Cells, 32 2309
4) Mulcahy Levy et al. (2014), Autophagy inhibition improves chemosensitivity in BRAFV600E brain tumors; Cancer Discov., 4 773