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Combrestatin A4 (CA4) is a potent inhibitor of tubulin polymerization and displays strong inhibitory activity on tumor cell growth. CA4 was shown to impede tumor growth in several cell lines including IMR32 (neuroblastoma), Hs746T (gastric carcinoma), CFPAC-1 (pancreatic carcinoma), and MCF-7 (breast cancer) with IC50 values of 2.16, 5.20, 3.46, and 18.47 nM, respectively. CA4 inhibits tubulin polymerization with an IC50 value of 2.2 μM. Combrestatin A4 is an inhibitor of β Tubulin.
1 Sun, L., Vasilevich, N.I., Fuselier, J.A., et al. Abilities of 3,4-diarylfuran-2-one analogs of combretastatin A-4 to inhibit both proliferation of tumor cell lines and growth of relevant tumors in nude mice. Anticancer Res 24 179-186 (2004). 2 Dey, P. Chromatin remodeling, cancer and chemotherapy. Current Medicinal Chemistry 13 2909-2919 (2006).
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