1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Tanshinone IIA (Synonyms: Dan Shen ketone)

Cat. No.: HY-N0135
Handling Instructions

Tanshinone IIA (Tan IIA) is one of the main fat-soluble compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.

For research use only. We do not sell to patients.
Tanshinone IIA Chemical Structure

Tanshinone IIA Chemical Structure

CAS No. : 568-72-9

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  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

Tanshinone IIA (Tan IIA) is one of the main fat-soluble compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.

IC50 & Target

VEGF/VEGFR2[1]

In Vitro

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-proliferative effects on A549 cells: the IC50 of Tanshinone IIA after 24, 48 and 72 h are 145.3, 30.95 and 11.49 μM, respectively. The CCK-8 assay is used to evaluate the proliferative activity of A549 cells treated with Tanshinone IIA (2.5-80 μM) for 24, 48 and 72 h, respectively. The CCK-8 results show that Tanshinone IIA can significantly inhibit A549 cell proliferation in a dose- and time-dependent manner. Obvious apoptosis and cell growth inhibition of A549 cells are observed after drug treatment for 48 h (concentrations used are approximately IC50 values: Tanshinone IIA 31 μM on A549). Western blotting finds that 48 h exposures to Tanshinone IIA (31 μM) in A549 cells, downregulates expression of VEGF and VEGFR2 protein in both drug treatment groups vs. vehicle[1]. Tanshinone IIA, one of the most abundant constituents of the root of Salvia miltiorrhiza, protects rat myocardium-derived H9C2 cells against apoptosis. Treatment of H9C2 cells with Tanshinone 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 inhibits angiotensin II (AngII)-induced apoptosis by downregulating the expression of phosphatase and tensin homolog (PTEN)[2]. Tanshinone IIA decreases the protein expression of EGFR, and IGFR blocking the PI3K/Akt/mTOR pathway in gastric carcinoma AGS cells[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01637675 The First Affiliated Hospital of Guangzhou Medical University|Jiangsu Carefree Pharmaceutical Co., Ltd.|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School|Guangdong General Hospital|Sir Run Run Shaw Hospital|The First Affiliated Hospital of Zhengzhou University|Dongguan People's Hospital|Second Affiliated Hospital of Xi'an Jiaotong University|Beijing Chao Yang Hospital|Beijing Anzhen Hospital|Qingdao University Pulmonary Hypertension|Pulmonary Arterial Hypertension|Cardiovascular Diseases|Lung Diseases|Tanshinone IIA Sulfonate May 2013 Phase 2|Phase 3
NCT02524964 Guangdong Provincial Hospital of Traditional Chinese Medicine Left Ventricular Remodeling|Acute Myocardial Infarction December 2015 Phase 4
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 3.3974 mL 16.9872 mL 33.9743 mL
5 mM 0.6795 mL 3.3974 mL 6.7949 mL
10 mM 0.3397 mL 1.6987 mL 3.3974 mL
Cell Assay
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

294.34

Formula

C₁₉H₁₈O₃

CAS No.

568-72-9

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Tanshinone IIA
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HY-N0135
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