Lexibulin

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Chemical Structure| 917111-44-5 同义名 : -
CAS号 : 917111-44-5
货号 : A225027
分子式 : C24H30N6O2
纯度 : 99%
分子量 : 434.53
MDL号 : MFCD18206787
存储条件:

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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
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

[1]Monaghan K, Khong T, Smith G, Spencer A. CYT997 causes apoptosis in human multiple myeloma. Invest New Drugs. 2011 Apr;29(2):232-8.

[2]Burns CJ, Fantino E, et al. CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol Cancer Ther. 2009 Nov;8(11):3036-45.

[3]Burns CJ, Fantino E, Phillips ID, et al. CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol Cancer Ther. 2009;8(11):3036-3045. doi:10.1158/1535-7163.MCT-09-0076