名称 | Tanshinone IIA |
描述 | Tanshinone IIA (Tanshinone B) is a diterpene quinone natural product that targets the protein kinase domain of VEGF/VEGFR2. Tanshinone IIA inhibits angiogenesis and exhibits anti-inflammatory, antioxidant, and therapeutic activities against coronary heart disease. |
细胞实验 | Tanshinone IIA (Tan IIA) is dissolved in DMSO (10 mM) and stored (in dark and -20°C), and serially diluted in a RPMI 1640 medium immediately prior to experiments[1]. A549 cells are counted in logarithmic phase and 6000 cells (90 μL volume) are placed in 96-well plates. 10 μL varying concentrations of Tanshinone IIA (final concentrations 80, 60, 40, 30, 20, 15, 10, 5 and 2.5 μM) and ADM (final concentrations 8, 4, 2, 1, 0.5 and 0.25 μM) are added into drug groups, while negative control group (vehicle group) is only added 10 μL DMSO or normal saline without Tanshinone IIA or ADM. Cells are incubated for an additional 2 h with CCK-8 reagent (100 μL/mL medium) and the absorbance is read at 450 nm using a microplate reader. Cell proliferation inhibition rates are calculated according to the following formula: the proliferation inhibition ratio (%)=1-[(A1-A4)/(A2-A3)]×100, where, A1 is the OD value of drug experimental group, A2 is the OD value of blank control group, A3 is the OD value of the RPMI1640 medium without cells, and A4 is the OD value of drugs with the same concentration as A1 but without cells. The IC50 value, which represents the concentration of the drug that demonstrates 50% of cell growth inhibition, is calculated by nonlinear regression analysis using GraphPad Prism software[1]. |
体外活性 | 方法: 人乳腺癌细胞 MCF-7 用 Tanshinone IIA (0.0625-1 µg/mL) 处理 5 天,使用 MTT assay 检测细胞活力。
结果: Tanshinone IIA 对细胞生长有剂量和时间依赖性的抑制作用,IC50 为 0.25 µg/mL,1 µg/mL 时最大抑制细胞生长 (>80%)。[1]
方法: 人乳腺癌细胞 MCF-7 用 Tanshinone IIA (5-20 µM) 处理 12-48 h,使使用 Flow cytometry 检测细胞凋亡。
结果: 在 Tanshinone IIA 的存在下观察到浓度依赖性的细胞凋亡诱导。[2] |
体内活性 | 方法: 为检测体内抗肿瘤活性,将 Tanshinone IIA (30 mg/kg) 注射给携带 MCF-7 肿瘤异种移植物的 BALB/c-nu 裸鼠,每周五次,持续两周。
结果: Tanshinone IIA 治疗显著减少了肿瘤的大小和重量。Tanshinone IIA 处理增强了体内 PARP 和 caspase-3 的切割。[2] |
存储条件 | Powder: -20°C for 3 years | Shipping with blue ice. |
溶解度 | DMSO : 2.94 mg/mL (10 mM), The compound is unstable in solution. Please use soon. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.29 mg/mL (0.99 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
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关键字 | inhibit | VEGFR | Vascular endothelial growth factor receptor | Tanshinone IIA | Inhibitor |
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