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Tubulin polymerization-IN-4

Tubulin polymerization-IN-4

产品编号 T61940

Tubulin polymerization-IN-4 是有效的微管蛋白聚合体 (tubulin polymerization) 抑制剂(IC50=4.6 μM)。Tubulin polymerization-IN-4 可以破坏微管蛋白聚合,将细胞周期阻滞在G2/M 期,诱导细胞凋亡 (apoptosis),抑制细胞的克隆发生和迁移。Tubulin polymerization-IN-4还可以破坏血管系统。

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Tubulin polymerization-IN-4
Tubulin polymerization-IN-4, CAS N/A
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 10-14周
50 mg ¥ 13,800 10-14周
100 mg ¥ 17,500 10-14周
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Tubulin polymerization-IN-4 (T61940)
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该分子属于定制产品。陶术拥有优秀的合成团队,经验和能力,可以为您提供高性价比的产品。但由于客观因素,研发中会存在小概率合成不成功的情况,还请理解,如您有任何问题,欢迎咨询,我们将竭诚为您服务。
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生物活性
化学信息
存储 & 溶解度
产品描述 Tubulin polymerization-IN-4 is an effective inhibitor of tubulin polymerization (IC50=4.6 μM)。 Tubulin polymerization-IN-4 can destroy tubulin polymerization, block cell cycle at G2/M phase, induce apoptosis, and inhibit cell cloning and migration. Tubulin polymerization-IN-4 can also damage the vascular system.
体外活性 Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751 [1]. Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM [1]. Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner [1]. Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube [1]. Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner [1]. Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells [1]. Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner [1]. Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner [1]. Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC 50 of 188 ± 16 μM in HK-2 cells [1]. Cell Proliferation Assay Cell Line: HeLa, SiHa and MS751 [1] Concentration: 0-1 μM Incubation Time: 48 hours Result: Exhibited sub-micromolar inhibitory activities against HeLa, SiHa and MS751 with IC 50 s of 0.09 ± 0.02 μM, 0.15 ± 0.01 μM, 0.11 ± 0.03 μM. Cell Cycle Analysis Cell Line: HeLa cells [1] Concentration: 0.1, 0.2 and 0.4 μM Incubation Time: 24 hours Result: Increased cell distribution to the G2/M phase in a concentration-dependent way, arresting 24.7%, 47.6% and 71.7% of the cells in this phase at 0.1, 0.2 and 0.4 μM, respectively. Apoptosis Analysis Cell Line: HeLa cells [1] Concentration: 0.1, 0.2 and 0.4 μM Incubation Time: 24 hours Result: Induced 35.9%, 66.4% and 84.4% of cell population undergoing apoptosis at 0.1 μM, 0.2 μM, 0.4 μM, respectively. Cell Cytotoxicity Assay Cell Line: HK-2 cells [1] Concentration: 0-200 μM Incubation Time: 24 hours Result: Exhibited good renal safety profile, with IC 50 of 188 ± 16 μM in HK-2 cells.
体内活性 Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD 50 over 1000 mg/kg [1]. Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg [1]. Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties [1]. Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice [1]. IP (30 mg/kg) T 1/2 (h) 1.56 ± 0.28 T max (h) 0.25 C max (μg/L) 6215 ± 308 AUC 0-t (μg/L·h) 5609 ± 347 AUC 0-∞ (μg/L·h) 5940 ± 347 V Z /F (L/kg) 11.35 ± 1.29 CL Z /F (L/h/kg) 5.05 ± 0.91 MRT (h) 1.77 ± 0.43
分子量 400.86
分子式 C21H21ClN2O4

存储

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

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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。

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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

Tubulin polymerization-IN-4 Inhibitor inhibitor inhibit

 

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