ABC294640 is an orally bioavailable, selective inhibitor of sphingosine kinase 2 (SPHK2 or SK2). Sphingosine kinases phosphorylate sphingosine producing the bioactive lipid sphingosine 1-phosphate which has roles in cell proliferation and cell motility. Sphingosine kinases are up-regulated in numerous forms of cancer and ABC294640, alone or in combination, has been shown to suppress growth in kidney, breast, liver, colon, and lung cancer cell lines.
References
Powered by Bioz1) M. B. Thomas, et al. “Phase I trial of ABC294640, a first-in-class sphingosine kinase-2 inhibitor” Mol. Cancer. Ther. 2013, 12, C62, DOI: 10.1158/1535-7163.TARG-13-C62.
2) K.J French, et al. “Pharmacology and antitumor activity of ABC294640, a selective inhibitor of sphingosine kinase-2.” J. Pharmacol. Exp. Ther. 2010, 333, 129-139.
3) M.M. Gestaut, et al. “Inhibition of sphingosine kinase-2 ablates androgen resistant prostate cancer proliferation and survival.” Pharmacol. Rep. 2014, 66, 174-178.
