Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 0.1 mg/mL (insoluble)
DMSO: 100 mg/mL (142.45 mM), sonification is recommended.
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Soblidotin 149606-27-9 Cytoskeletal Signaling Microtubule Associated TZT1027 Auristatin PE inhibit Microtubule/Tubulin Inhibitor TZT-1027 TZT 1027 inhibitor