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Lexibulin {[allProObj[0].p_purity_real_show]}

货号:A225027

Lexibulin can potently inhibit microtubule polymerization with vascular-disrupting, and potential antineoplastic activities.

Lexibulin 化学结构 CAS号:917111-44-5
Lexibulin 化学结构
CAS号:917111-44-5
Lexibulin 3D分子结构
CAS号:917111-44-5
Lexibulin 化学结构 CAS号:917111-44-5
Lexibulin 3D分子结构 CAS号:917111-44-5
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Lexibulin 纯度/质量文件 产品仅供科研

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Lexibulin 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].

Lexibulin 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

Lexibulin 实验方案

计算器
存储液制备 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

Lexibulin 技术信息

CAS号917111-44-5
分子式C24H30N6O2
分子量 434.53
SMILES Code O=C(NC1=CC=C(C2=NC=C(C)C(N[C@H](C3=CC=CN=C3)CCC)=N2)C=C1OC)NCC
MDL No. MFCD18206787
别名
运输蓝冰
InChI Key MTJHLONVHHPNSI-IBGZPJMESA-N
Pubchem ID 11351021
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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