Fosbretabulin is a natural cis-stilbene that interferes with cellular tubulin dynamics and selectively destroys tumor blood vessels.

Combretastatin A4 (CA4) is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM).

Ombrabulin hydrochloride is a synthetic, selective CA-4 phosphate ester or derivative of Ombrabulin to disrupt the tubulin cytoskeleton of endothelial cells and has antivascular effects. Ombrabulin is a tubulin polymerizing inhibitor, a member of the combretastatin A-4 compound class, which is a water-soluble tubulin depolymerizing tumor vascularizing compound.

STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, in an aggressive syngeneic model, demonstrated superior tumor growth inhibition and a positive therapeutic index relative to combretastatin A-4 phosphate (CA4P).

HYS-32, as an analog of combretastatin A-4, can exert by enhancing connexin43 expression.

isoCA-4 is a Combretastatin A4 derivative. isoCA-4 is a tubulin polymerization inhibitor with anti-proliferative activities [1].

YK-5-252 is a dual action combretastatin A-4 (CA-4) prodrug which releases CA-4 through a disulfide bond cleavage mechanism and contains a near-infrared (NIR) fluorophore.