9-Methoxyellipticine

9-Methoxyellipticine is an alkaloid and a derivative of the DNA intercalating agent ellipticine that has been found in O. maculata and has anticancer activity.^1,2 It intercalates into DNA and is an inhibitor of wild-type c-Kit and c-Kit containing the D816V activating mutation (c-Kit^D816V; IC₅₀s = 0.8 and 0.6 µM, respectively).^2,3 9-Methoxyellipticine inhibits proliferation of Ba/F3 cells in the presence of the c-Kit ligand SCF and Ba/F3 cells expressing c-Kit^D816V (IC₅₀s = 0.5 and 0.3 µM, respectively).² It also increases survival in a variety of rodent tumor models.¹

1.Svoboda, G.H., Poore, G.A., and Montfort, M.L.Alkaloids of Ochrosia maculata Jacq. (Ochrosia borbonica Gmel.). Isolation of the alkaloids and study of the antitumor properties of 9-methoxyellipticineJ. Pharm. Sci.57(10)1720-1725(1968) 2.VendÔme, J., Letard, S., Martin, F., et al.Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinasesJ. Med. Chem.48(20)6194-6201(2005) 3.Festy, B., Poisson, J., and Paoletti, C.A new DNA intercalating drug: Methoxy-9-ellipticineFEBS Lett.17(2)321-323(1971)