Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MY-875 is a potent microtubulin polymerization inhibitor that competes at colchicine binding sites, exhibiting an IC50 value of 0.92 μM. It effectively suppresses microtubulin polymerization, exerting its inhibitory effect. Additionally, MY-875 exerts its biological impact by activating the Hippo pathway, inducing apoptosis, and displaying commendable anticancer activity [1].
产品描述 | MY-875 is a potent microtubulin polymerization inhibitor that competes at colchicine binding sites, exhibiting an IC50 value of 0.92 μM. It effectively suppresses microtubulin polymerization, exerting its inhibitory effect. Additionally, MY-875 exerts its biological impact by activating the Hippo pathway, inducing apoptosis, and displaying commendable anticancer activity [1]. |
体外活性 | MY-875 (0-80 μM, 48 h) has significant anti-proliferative activity against cancer cells [1]. MY-875 (1-10 μM) can inhibit microtubule protein polymerization with an IC 50 value of 0.92 μM while inhibiting alkylation of β-tubulin and the formation of EBI-β-tubulin adduct bands in a dose-dependent manner [1]. MY-875 (0-45 nM, 48 h) can induce the phosphorylation state of MST (Ste20-like kinases) and LATS (large tumor suppressor kinases), leading to YAP (Yes-associated protein) degradation in a dose-dependent manner [1]. MY-875 (0-45 nM, 24 h) significantly inhibits cell colony-forming ability, arrests cells in the G2/M phase and induces cell apoptosis in a dose-dependent manner [1]. Cell Proliferation Assay [1] Cell Line: MGC-803, HCT-116, KYSE450, HGC-27, SGC-7901cell lines Concentration: 0-80 μM Incubation Time: 48 hours Result: Inhibited the proliferation of MGC-803, HCT-116, KYSE450, HGC-27 and SGC-7901 cells with the IC 50 values of 0.027, 0.055, 0.067, 0.033 and 0.025 μM, respectively. Showed strong inhibitory effect on other tumor cell lines with the IC 50 values less than 0.1 μM, such as DU145, A549, MCF-7, etc. Cell Cycle Analysis [1] Cell Line: MGC-803, SGC-7901 cell lines Concentration: 0-45 nM Incubation Time: 24 hours Result: Increased the percentage of cells in G2/M phase from 19.38% to 76.97% in MGC-803 cells and from 7.04% to 80.89% in SGC-7901 cells, respectively at 45 nM. Apoptosis Analysis [1] Cell Line: MGC-803, SGC-7901 cell lines Concentration: 0-45 nM Incubation Time: 48 hours Result: Induced apoptotic cells from 21.96% to 76.08% in MGC-803 cells and from 9.28% to 63.51% in SGC-7901 cells, respectively at 45 nM. Reduced expression of anti-apoptotic proteins c-IAP1, Bcl-xL and Mcl-1. |
分子量 | 387.43 |
分子式 | C21H25NO6 |
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。
MY-875 Inhibitor inhibitor inhibit