化合物Soblidotin T14350

Product Introduction
Bioactivity


英文名: Soblidotin

描述: 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。

体外活性: Soblidotin (Auristatin PE) 抑制多个肿瘤细胞系的生长，并诱导依赖于caspase-3的凋亡。Soblidotin (Auristatin PE) 还在Vincristine、Docetaxel和Paclitaxel抗性肿瘤中表现出抗肿瘤活性，这使其成为一种潜在的化疗药物，用于对其他微管抑制剂无反应的肿瘤[2]。此外，Soblidotin (Auristatin PE) 对表达P-糖蛋白的结肠癌H116细胞系和表达乳腺癌抗药蛋白阳性的肺癌PC-6细胞系展现出抗肿瘤活性，其功效超过Vincristine、Paclitaxel和Docetaxel [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].

存储条件: 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)


关键字: TZT1027 | Soblidotin | inhibit | Microtubule/Tubulin | Inhibitor | TZT 1027

相关产品: Triclabendazole | ELR510444 | 4'-Demethylepipodophyllotoxin | Dolastatin 10 | Tirbanibulin | KHS 101 | Methylene Blue trihydrate | Mivobulin | Fosbretabulin Disodium | S516

相关库: ReFRAME Related Library | Anti-Cancer Drug Library | Microtubule-Targeted Compound Library | Clinical Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途