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| 10mg |
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| 25mg |
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Purity: ≥98%
Cryptotanshinone (also called Cryptotanshinon; Tanshinone c), a naturally occuring compound found from the roots of Salvia miltiorrhiza Bunge (Danshen, a Chinese medicinal plant), is a potent STAT3 inhibitor with potential antitumor activity. It inhibits STAT3 with an IC50 of 4.6 μM in a cell-free assay.
| ln Vitro |
Compared to tanshinone IIA, which shows negligible effect, cryptotanshinone strongly suppresses STAT3-dependent luciferase activity, the phosphorylation of Tyr705 on STAT3, and the dimerization of STAT3. In DU145 cells, cryptotanshinone (7 μM) significantly inhibits JAK2 phosphorylation with an IC50 of approximately 5 μM while having no effect on the phosphorylation of upstream kinases c-Src and EGFR. This suggests that the inhibition of STAT3 Tyr705 phosphorylation may be the result of a direct mechanism, most likely through binding to the SH2 domain of STAT3. At a GI50 of 7 μM, cryptotanshinone dramatically suppresses the growth of DU145 prostate cancer cells that possess constitutively active STAT3. This is achieved by inhibiting STAT3 activity, which causes cyclin D1, Bcl-xL, and survivin to be down-regulated, which then accumulates in the G0-G1 phase. Less growth inhibition is seen by cryptotanshinone in PC3, LNCaP, and MDA-MB-468 cells[1]. As evidenced by a considerable decrease in T and a rise in P levels in the culture media, cryptotanshinone considerably attenuates the in vitro hormonal effects of DEX on ovaries. In the ovaries treated with DEX, cryptotanshinone markedly raises the levels of phosphorylated AKT2 and GSK3β[2]. In primary CML cells as well as imatinib-sensitive and -resistant CML cell lines, cotreatment with imatinib and cryptotanshinone has a strong synergistic killing effect[3].
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| ln Vivo |
In every tissue from the DEX-treated mice that is analyzed, cryptotanshinone dramatically raises 2-deoxy-D-[1,2-3H]-glucose absorption and reverses the ovarian IR. The plasma E2 and P levels as well as the ovulation rate are both markedly decreased by cryptotanshinone[2]. In a dose-dependent manner, treatment of cryptotanshinone dramatically lowers the body weight and food intake of diet-induced obese (DIO) mice and ob/ob mice (C57BL/6J-Lepob). Compared to control mice, adipose tissue fat is significantly reduced, blood triglyceride and cholesterol levels are significantly lowered, and skeletal muscle AMPK activity is 2.5–3 times higher in response to cryptotanshinone. After three days and continuing for the duration of the monitoring period, oral treatment of 600 mg/kg/day of Cryptotanshinone causes significant drops in blood glucose levels in ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats[4].
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| References |
[1]. Shin DS, et al. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells. Cancer Res. 2009 Jan 1;69(1):193-202.
[2]. Huang Y, et al. Cryptotanshinone reverses ovarian insulin resistance in mice through activation of insulin signaling and the regulation of glucose transporters and hormone synthesizing enzymes. Fertil Steril. 2014 Aug;102(2):589-596.e4. [3]. Ge Y, et al. Cryptotanshinone acts synergistically with imatinib to induce apoptosis of human chronic myeloid leukemia cells. Leuk Lymphoma. 2014 Jun 25:1-9. [4]. Kim EJ, et al. Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase. Mol Pharmacol. 2007 Jul;72(1):62-72. Epub 2007 Apr 11 |
| Molecular Formula |
C19H20O3
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| Molecular Weight |
296.36
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| CAS # |
35825-57-1
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| SMILES |
O1C([H])([H])[C@]([H])(C([H])([H])[H])C2C(C(C3=C(C([H])=C([H])C4=C3C([H])([H])C([H])([H])C([H])([H])C4(C([H])([H])[H])C([H])([H])[H])C1=2)=O)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.83 mg/mL (2.80 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 2mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3743 mL | 16.8714 mL | 33.7427 mL | |
| 5 mM | 0.6749 mL | 3.3743 mL | 6.7485 mL | |
| 10 mM | 0.3374 mL | 1.6871 mL | 3.3743 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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