中文名称: | Soblidotin | ||||
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英文名称: | Soblidotin | ||||
别名: | 舒碧利婷 Auristatin PE; TZT-1027 | ||||
CAS No: | 149606-27-9 | 分子式: | C39H67N5O6 | 分子量: | 701.98 |
CAS No: | 149606-27-9 | ||||
分子式: | C39H67N5O6 | ||||
分子量: | 701.98 |
基本信息
产品编号:S10786 |
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产品名称:Soblidotin |
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CAS: |
149606-27-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
4℃ |
两年 |
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分子量 |
701.98 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.4245mL |
7.1227mL |
14.2454mL |
5mM |
0.2849mL |
1.4245mL |
2.8491mL |
10mM |
0.1425mL |
0.7123mL |
1.4245mL |
生物活性
产品描述 |
一种新型合成的 Dolastatin 10衍生物,抑制剂微管 (tubulin) 聚合。 |
靶点/IC50 |
Tubulin |
体外研究 |
Soblidotin (Auristatin PE) is a novel synthetic dolastatin 10 derivative that inhibits tubulin polymerization. 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. Soblidotin (Auristatin PE) is a synthetic analog of dolastatin 10 which 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 which do not respond to other microtubule inhibitors. |
体内研究 |
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 Dolastatin10,Cisplatin,Vincristine,and 5-Fluorouracil. Furthermore,in xenograft models, Auristatin PE reduces intratumoral blood perfusion 1 to >24h after its administration,thereby producing hemorrhagic necrosis of the tumors. 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.Mice bearing subcutaneous HT-29 tumors (200mm3) are dosed every 7 days with Auristatin PE (0.5 or 1.0mg/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.Coadministration of Auristatin PE does not interfere with the PD184352-induced suppression of ERK1/2 phosphorylation.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. |
推荐实验方法(仅供参考)
动物实验: |
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Mice Soblidotin (Auristatin PE) and Vinorelbine are dissolved in 0.05M sodium lactate buffer (pH 4.5) and in PBS, respectively.Mice are treated every 7 d with PD184352 (200mg/kg) or vehicle by oral administration (four times per day, every 6h) and with Auristatin PE (0.25-2.5mg/kg), Vinorelbine (5-20mg/kg), or vehicle by i.v. injection (once per day, 1h after the first PD184352 administration). Tumor volume is measured with digital calipers and calculated according to the following formula: (longest diameter)×(shortest diameter)2/2. Body weight, tumor volume, and toxicities are noted every 2 to 4 d for the duration of the experiment. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )