Tubulin inhibitor 11,99.92%

产品编号:Bellancom-152156| CAS NO:2366260-33-3| 分子式:C22H23N3O3S| 分子量:409.50

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-152156
1500.00 杭州 北京(现货)
Bellancom-152156
2500.00 杭州 北京(现货)
Bellancom-152156
5500.00 杭州 北京(现货)
Bellancom-152156
8500.00 杭州 北京(现货)
Bellancom-152156
13500.00 杭州 北京(现货)

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Tubulin inhibitor 11

产品介绍 Tubulin inhibitor 11 是一种有效的具有口服活性的微管蛋白 (tubulin) 抑制剂。Tubulin inhibitor 11 靶向微管蛋白上的秋水仙碱结合位点,抑制微管蛋白聚合,促进有丝分裂阻断和细胞凋亡 (apoptosis)。
生物活性

Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.

体外研究

Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis.
Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC50 of 8 nM.
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

Cell Line: DU145 cells
Concentration: 0.01 μM, 0.03 μM, and 0.1 μM
Incubation Time: 12 hours
Result: Caused cell cycle arrest at G2/M phase.

Apoptosis Analysis

Cell Line: DU145 cells
Concentration: 0.03 μM, 0.1 μM, and 0.3 μM
Incubation Time: 48 hours
Result: Induced cancer cell apoptosis.

Western Blot Analysis

Cell Line: DU145 cells
Concentration: 0.01 μM, 0.03 μM, and 0.1 μM
Incubation Time: 12 hours
Result: Reduced cdc2 phosphorylation and increased cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.
体内研究
(In Vivo)

Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells
Dosage: 5 mg/kg, 10 mg/kg
Administration: p.o; once daily
Result: Effectively suppressed tumor growth.
体内研究

Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells
Dosage: 5 mg/kg, 10 mg/kg
Administration: p.o; once daily
Result: Effectively suppressed tumor growth.
体内研究

Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells
Dosage: 5 mg/kg, 10 mg/kg
Administration: p.o; once daily
Result: Effectively suppressed tumor growth.
性状Solid
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (244.20 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4420 mL 12.2100 mL 24.4200 mL
5 mM 0.4884 mL 2.4420 mL 4.8840 mL
10 mM 0.2442 mL 1.2210 mL 2.4420 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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