生物活性 | |||
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描述 | Microtubules are highly dynamic polymers of tubulin that play an important role in mitosis, intracellular transport, and motility. Lexibulin is a synthetic, orally-active tubulin polymerization inhibitor with an IC50 value of ~3μM. It inhibits the proliferation of a panel of cancer cell lines with IC50 values ranging from 10 to 100nM. Treatment of A549 cells with 1μM lexibulin led to rapid destruction of the microtubule network and the accumulation of tubulin in plaques. Incubation of A431 cells with 1μM lexibulin increased the proportion of cells in G2-M at 15 and 24h after the exposure compared to the vehicle-treated group (38% vs. 15%, 43% vs. 19%, respectively). Lexibulin (100nM and 1μM) increased the permeability of human umbilical vein endothelial cell monolayer as early as 1h post-exposure and the IC50 value of lexibulin was ~80nM. In a mouse model of colorectal liver metastases, a single dose of lexibulin (7.5mg/kg, i.p.) significantly decreased blood flow in liver metastases at 6h after treatment[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.51mL 2.30mL 1.15mL |
23.01mL 4.60mL 2.30mL |
参考文献 |
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