Tanshinone-IIA-Dan-Shen-ketone-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETanshinone IIACat. No.: HY-N0135CAS No.: 568-72-9Synonyms: Dan Shen ketone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 m

2、M; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration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

3、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。IC50 & Target VEGF/VEGFR2 11/3 Master of Small Molecules 您边的抑制剂师www.MedChemE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 inhibitin

4、g tumor cell invasion and transfer. Tanshinone IIA has anti-proliferative effects on A549 cells: the IC50 of Tanshinone IIA after 24, 48 and 72 h are 145.3, 30.95 and11.49 M, respectively. The CCK-8 assay is used to evaluate the proliferative activity of A549 cells treatedwith Tanshinone IIA (2.5-80

5、 M) for 24, 48 and 72 h, respectively. The CCK-8 results show that TanshinoneIIA can significantly inhibit A549 cell proliferation in a dose- and time-dependent manner. Obvious apoptosisand cell growth inhibition of A549 cells are observed after drug treatment for 48 h (concentrations used areapprox

6、imately IC50 values: Tanshinone IIA 31 M on A549). Western blotting finds that 48 h exposures toTanshinone IIA (31 M) in A549 cells, downregulates expression of VEGF and VEGFR2 protein in both drugtreatment groups vs. vehicle 1. Tanshinone IIA, one of the most abundant constituents of the root of Sa

7、lviamiltiorrhiza, protects rat myocardium-derived H9C2 cells against apoptosis. Treatment of H9C2 cells withTanshinone 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. T

8、anshinone IIAinhibits angiotensin II (AngII)-induced apoptosis by downregulating the expression of phosphatase and tensinhomolog (PTEN) 2. Tanshinone IIA decreases the protein expression of EGFR, and IGFR blocking thePI3K/Akt/mTOR pathway in gastric carcinoma AGS cells 3.PROTOCOLCell Assay 1 A549 ce

9、lls are counted in logarithmic phase and 6000 cells (90 L volume) are placed in 96-well plates. 10 L varying concentrations of Tanshinone IIA (final concentrations 80, 60, 40, 30, 20, 15, 10, 5 and 2.5 M) andADM (final concentrations 8, 4, 2, 1, 0.5 and 0.25 M) are added into drug groups, while nega

10、tive controlgroup (vehicle group) is only added 10 L DMSO or normal saline without Tanshinone IIA or ADM. Cells areincubated for an additional 2 h with CCK-8 reagent (100 L/mL medium) and the absorbance is read at 450nm using a microplate reader. Cell proliferation inhibition rates are calculated ac

11、cording to the followingformula: the proliferation inhibition ratio (%)=1-(A1-A4)/(A2-A3)100, where, A1 is the OD value of drugexperimental group, A2 is the OD value of blank control group, A3 is the OD value of the RPMI1640 mediumwithout cells, and A4 is the OD value of drugs with the same concentr

12、ation as A1 but without cells. The IC50value, which represents the concentration of the drug that demonstrates 50% of cell growth inhibition, iscalculated by nonlinear regression analysis using GraphPad Prism software 1.MCE has not independently confirmed the accuracy of these methods. They are for

13、reference only.户使本产品发表的科研献 J Pharm Pharmacol. 2018 Oct;70(10):1369-1377.See more customer validations on HYPERLINK / 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 lung cancer A549

14、cell line. Acta Pharm Sin B. 2015 Nov;5(6):554-63.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. Zhang Z, et al. Tanshinone IIA inhibits apoptosis in the myocardium by inducing microRNA-152-3p expression and therebydownregulating PTEN. Am J Transl 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 gastriccarcinoma AGS cells both in vitro and in vivo. Oncol Rep. 2016