Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Anticancer agent 82 是 FiVe1 衍生物,是一种口服有效的选择性抗癌剂。FiVe1 能够结合 III 型中间丝蛋白vimentin(VIM),诱导 Ser56 过度磷酸化,导致有丝分裂的选择性中断和转化表达 VIM 的间充质癌细胞的多核化。Anticancer agent 82 比 FiVe1 表现出更好的口服利用度和药代动力学特征。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,100 | 5日内发货 | ||
100 mg | ¥ 9,967 | 6-8周 |
产品描述 | Anticancer agent 82 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin ( VIM ), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Anticancer agent 82 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 [1]. |
体外活性 | Anticancer agent 82 (compound 4e) (0-10 mM; 72 h) inhibits a marked improvement in potency with an IC 50 value of 44 nM against HT-1080 fibrosarcoma, better than than FiVe1 (IC 50 =1.6 μM, HT-1080) [1]. Anticancer agent 82 (0.1 μM; 24 h) induces phosphorylation of VIM at Ser56 [1]. Anticancer agent 82 (100 μM; sampled at 0, 5, 15, 30, 45, and 60 min) exhibits poor stability with 0.0% remaining after 60 min of incubation in mouse liver microsome [1]. Cell Viability Assay [1] Cell Line: HT-1080, RD, and MCF-7 cells Concentration: 0-10 mM Incubation Time: 72 hours Result: Inhibited HT-1080, RD, and MCF-7 cells with IC 50 s of 44 nM, 61 nM, and 49 nM, respectively. |
体内活性 | Anticancer agent 82 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1 [1]. Pharmacokinetic properties of Anticancer agent 82 in mice [1] Route Dose (mg/kg) AUC 0-last (ng·h/mL) AUC 0-inf (ng·h/mL) T 1/2 (h) T max (h) T last (h) C max (ng/mL) 4e PO 10 371.33 534.33 4.68 0.67 8 154.67 4e IP 1 208.33 211.33 0.59 0.25 4 197.00 Five1 PO 25 309.78 339.21 4.57 0.5 18 110.43 |
分子量 | 389.28 |
分子式 | C19H18Cl2N4O |
CAS No. | 2319587-80-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Anticancer agent 82 2319587-80-7 Inhibitor inhibitor inhibit