Sabizabulin

Sabizabulin is an inhibitor of tubulin polymerization.¹ It inhibits bovine tubulin polymerization in a cell-free assay when used at concentrations of 5 and 10 µM. Sabizabulin inhibits the growth of A375 and WM164 melanoma, LNCaP, PC3, and DU145 prostate cancer cells, as well as paclitaxel-resistant PC3 cells (IC₅₀s = 3.2, 5.3, 2.8, 3.7, 3.9, and 3.7 nM, respectively).¹ It reduces the migration and invasion of MDA-MB-231 and MDA-MB-468 breast cancer cells when used at a concentration of 8 nM, as well as decreases the migration rate in wound-healing assays using the same cells at 16 nM.² Sabizabulin (50 nM) induces cell cycle arrest at the G₂/M phase in MDA-MB-231 cells and the G₂ phase in MDA-MB-468 cells, as well as apoptosis in these same cells. It decreases tumor volume, tumor weight, and angiogenesis, as well as increases tumor necrosis, without affecting body weight, in an MDA-MB-231 mouse xenograft model when administered at doses of 5, 10, and 12.5 mg/kg. Sabizabulin (10 mg/kg) reduces the number of lung, liver, and kidney metastases in an MDA-MB-231 mouse xenograft model of metastasis.

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1. Chen, J., Ahn, S., Wang, J., et al. Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. J. Med. Chem. 55(16), 7285-7289 (2012).

2. Deng, S., Krutilina, R.I., Wang, Q., et al. An orally available tubulin inhibitor, VERU-111, suppresses triple-negative breast cancer tumor growth and metastasis and bypasses taxane resistance. Mol. Cancer Ther. 19(2), 348-363 (2020).