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Soblidotin

Soblidotin

产品编号 T14350   CAS 149606-27-9
别名: Auristatin PE, TZT-1027

Soblidotin (TZT-1027) 是一种微管蛋白聚合抑制剂。它也是一种新型合成的 Dolastatin 10 衍生物。

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Soblidotin Chemical Structure
Soblidotin, CAS 149606-27-9
规格 价格/CNY 货期 数量
1 mg ¥ 1,150 现货
5 mg ¥ 2,890 现货
10 mg ¥ 4,160 现货
25 mg ¥ 6,680 现货
50 mg ¥ 8,920 现货
1 mL * 10 mM (in DMSO) ¥ 3,990 现货
产品目录号及名称: Soblidotin (T14350)
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纯度: 97.48%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Soblidotin (TZT-1027) (Auristatin PE) is an inhibitor of tubulin polymerization. It is also a novel synthetic Dolastatin 10 derivative.
体外活性 Soblidotin (Auristatin PE) inhibits the growth of several tumoral cell lines and induces caspase-3-dependent apoptosis. Soblidotin (Auristatin PE) also shows antitumoral activity in Vincristine-, Docetaxel-, and Paclitaxel-resistant tumors, which makes it a potential chemotherapy drug for use in tumors that do not respond to other microtubule inhibitors [2]. Soblidotin (Auristatin PE) exhibits antitumor activity against p-glycoprotein-overexpressing cell lines established from colon cancer H116 and breast cancer-resistant protein-positive cell lines established from lung cancer PC-6 and is more potent than Vincristine, Paclitaxel, and Docetaxel against these cell lines [1].
体内活性 Auristatin PE (Soblidotin) shows antivascular effects in tumoral models overexpressing VEGF and in murine colon tumors, with an increase in vascular permeability, vessel closure, and widespread hemorrhage [2]. Intravenous injection of Auristatin PE (TZT-1027) has been shown to potently inhibit the growth of P388 leukemic cells and several solid tumors in mice and to prolong the survival of the animals, and its antitumor efficacy has been shown to be superior or comparable to that of the reference agents Dolastatin 10, Cisplatin, Vincristine, and 5-Fluorouracil. Coadministration of Auristatin PE does not interfere with the PD184352-induced suppression of ERK1/2 phosphorylation. Furthermore, in xenograft models, Auristatin PE reduces intratumoral blood perfusion 1 to >24 h after its administration, thereby producing hemorrhagic necrosis of the tumors [1]. Mice bearing subcutaneous HT-29 tumors (200 mm3) are dosed every 7 days with Auristatin PE (0.5 or 1.0 mg/kg) for a total of four cycles. Under such conditions, Auristatin PE (TZT-1027) inhibits the growth of HT-29 xenografts in a dose-dependent manner. Immunostaining for Ki-67 as a marker for proliferating cells confirmed that the number of such cells in tumor sections is decreased greatly at 24 hours after the initial dosing with PD184352 compared with that apparent for vehicle-treated tumors. Auristatin PE treatment alone increases the number of TUNEL-positive cells in HT-29 xenografts by 24 hours in a dose-dependent manner, and this effect is enhanced by coadministration of PD184352 [3].
别名 Auristatin PE, TZT-1027
分子量 701.98
分子式 C39H67N5O6
CAS No. 149606-27-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 0.1 mg/mL (insoluble)

DMSO: 100 mg/mL (142.45 mM), sonification is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4245 mL 7.1227 mL 14.2454 mL 35.6136 mL
5 mM 0.2849 mL 1.4245 mL 2.8491 mL 7.1227 mL
10 mM 0.1425 mL 0.7123 mL 1.4245 mL 3.5614 mL
20 mM 0.0712 mL 0.3561 mL 0.7123 mL 1.7807 mL
50 mM 0.0285 mL 0.1425 mL 0.2849 mL 0.7123 mL
100 mM 0.0142 mL 0.0712 mL 0.1425 mL 0.3561 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Yamamoto N, et al. Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative and inhibitor of tubulin polymerization, given weekly to advanced solid tumor patients for 3 weeks. Cancer Sci. 2009 Feb;100(2):316-21. 2. Fanale D, et al. Stabilizing versus destabilizing the microtubules: a double-edge sword for an effective cancer treatment option? Anal Cell Pathol (Amst). 2015;2015:690916. 3. Watanabe K, et al. Blockade of the extracellular signal-regulated kinase pathway enhances the therapeutic efficacy of microtubule-destabilizing agents in human tumor xenograft models. Clin Cancer Res. 2010 Feb 15;16(4):1170-8.
PE859 Cephalomannine Mebendazole Verubulin Plinabulin Combretastatin A-1 Mc-MMAE 7-epi-Taxol

相关化合物库

该产品包含在如下化合物库中:
微管靶向化合物库 抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 ReFRAME 相关化合物库 药物功能重定位化合物库 抑制剂库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Soblidotin 149606-27-9 Cytoskeletal Signaling Microtubule Associated TZT1027 Auristatin PE inhibit Microtubule/Tubulin Inhibitor TZT-1027 TZT 1027 inhibitor

 

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