ABC294640 (Opaganib) 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.
Categories | Biochemical Reagents |
---|---|
Filter | Inhibitor, Sphingolipid |
CAS Number | 915385-81-8 |
Molecular Formula | C23H25ClN2O |
Molecular Weight (g/mol) | 380.91 |
Purity | >98% |
Storage | -20 °C or below |
Shipping Temp | Room Temperature |
1) 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.
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