丹参酮 IIA作用机制 - Medchemexpress - MCE中国

1、Product Data SheetTanshinone IIACat. No.: HY-N0135CAS No.: 568-72-9分式: CHO分量: 294.34作靶点: VEGFR作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 years* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 DMSO : 3.85 mg/mL (13.08 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcent

2、ration制备储备液1 mM 3.3974 mL 16.9872 mL 33.9743 mL5 mM 0.6795 mL 3.3974 mL 6.7949 mL10 mM 0.3397 mL 1.6987 mL 3.3974 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现现配，即刻使.BIOLOGICAL ACTIVITY物活性 Tanshinone IIA (Tan IIA)红根丹参根系中的主 脂溶性组合物之。Tanshinone IIA 可以通过靶向 VEGF/VEGFR2 的蛋激酶结构域来抑制管成。IC & Target VEGF/VEG

3、FR21体外研究The anti-tumor effect of Tanshinone IIA includes inhibiting tumor cell proliferation, disturbing tumor cell cycle,promoting tumor cell apoptosis, and inhibiting tumor cell invasion and transfer. Tanshinone IIA has anti-proliferativeeffects on A549 cells: the IC50 of Tanshinone IIA after 24,

4、48 and 72 h are 145.3, 30.95 and 11.49 M, respectively. TheCCK-8 assay is used to evaluate the proliferative activity of A549 cells treated with Tanshinone IIA (2.5-80 M) for 24,48 and 72 h, respectively. The CCK-8 results show that Tanshinone IIA can significantly inhibit A549 cell proliferationin

5、a dose- and time-dependent manner. Obvious apoptosis and cell growth inhibition of A549 cells are observed afterdrug treatment for 48 h (concentrations used are approximately IC50 values: Tanshinone IIA 31 M on A549). WesternPage 1 of 2 www.MedChemEblotting finds that 48 h exposures to Tanshinone II

6、A (31 M) in A549 cells, downregulates expression of VEGF andVEGFR2 protein in both drug treatment groups vs. vehicle1. Tanshinone IIA, one of the most abundant constituentsof the root of Salvia miltiorrhiza, protects rat myocardium-derived H9C2 cells against apoptosis. Treatment of H9C2cells with Ta

7、nshinone IIA inhibits angiotensin II-induced apoptosis by downregulating the expression of PTEN(phosphatase and tensin homolog), a tumor suppressor that plays a critical role in apoptosis. Tanshinone IIA inhibitsangiotensin II (AngII)-induced apoptosis by downregulating the expression of phosphatase

8、 and tensin homolog(PTEN)2. Tanshinone IIA decreases the protein expression of EGFR, and IGFR blocking the PI3K/Akt/mTOR pathway ingastric carcinoma AGS cells3.PROTOCOLCell Assay 1 A549 cells are counted in logarithmic phase and 6000 cells (90 L volume) are placed in 96-well plates. 10 L varyingconc

9、entrations of Tanshinone IIA (final concentrations 80, 60, 40, 30, 20, 15, 10, 5 and 2.5 M) and ADM (finalconcentrations 8, 4, 2, 1, 0.5 and 0.25 M) are added into drug groups, while negative control group (vehicle group) isonly added 10 L DMSO or normal saline without Tanshinone IIA or ADM. Cells a

10、re incubated for an additional 2 hwith CCK-8 reagent (100 L/mL medium) and the absorbance is read at 450 nm using a microplate reader. Cellproliferation inhibition rates are calculated according to the following formula: the proliferation inhibition ratio(%)=1-(A1-A4)/(A2-A3)100, where, A1 is the OD

11、 value of drug experimental group, A2 is the OD value of blankcontrol group, A3 is the OD value of the RPMI1640 medium without cells, and A4 is the OD value of drugs with thesame concentration as A1 but without cells. The IC50 value, which represents the concentration of the drug thatdemonstrates 50

12、% of cell growth inhibition, is calculated by nonlinear regression analysis using GraphPad Prismsoftware1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Chem-Biol Interact. 2020 Feb. Eur J Pharmacol. 2020 May. J Pharm Pharmacol. 2018 Oct;70

13、(10):1369-1377.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Xie J, et al. The antitumor effect of tanshinone IIA on anti-proliferation and decreasing VEGF/VEGFR2 expression on the human non-small cell lungcancer A549 cell line. Acta Pharm Sin B. 2015 Nov;5(6):554-

14、63.2. Zhang Z, et al. Tanshinone IIA inhibits apoptosis in the myocardium by inducing microRNA-152-3p expression and thereby downregulating PTEN. Am JTransl Res. 2016 Jul 15;8(7):3124-32.3. Su CC, et al. Tanshinone IIA decreases the protein expression of EGFR, and IGFR blocking the PI3K/Akt/mTOR pathway in gastric carcinoma AGS cellsboth in vitro and in vivo. Oncol Rep. 2016 Aug;36(2):1173-9.McePdfHeightPage 2 of 3 www.Me