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| 5mg |
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| 25mg |
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Purity: ≥98%
Triptolide (also known as NSC 163062), a diterpene triepoxide, is an immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. Ovarian cancer cells SKOV3 and A2780 were treated with triptolide at a concentration of 15 nM, which prevented the cells' invasion and migration. In ovarian cancer cells, triptolide reduced the expression of MMP7 and MMP19 in a dose-dependent manner from 0 to 15 nM. Additionally, triptolide increased the expression of E-cadherin in ovarian cancer cells, which had an impact on cell invasion and migration.
| Targets |
MDM-2/p53 (IC50 = 47-73 nM); HSP90
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| ln Vitro |
Triptolide is a diterpene triepoxide with strong anti-inflammatory and immunosuppressive properties. The purine-box/nuclear factor and NF-κB mediated transcription activation of IL-2 in activated T cells is shown to be inhibited by triptolide. [1] At incredibly low concentrations (2–10 ng/mL), triptolide prevents the growth and colony formation of tumor cells. Triptolide inhibits the growth of HL-60 leukemia cell line, stomach, and breast cancer cells. By inhibiting NF-κB activation and making tumor cells more susceptible to TNF-&alpha-induced programmed cell death, triptolide causes apoptosis in tumor cells. [2]
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| ln Vivo |
In animal models, triptolide and cyclosporin A work together to promote graft survival and prevent graft versus host disease after allogeneic bone marrow transplants. Additionally, by suppressing the induction of c-IAP2 and c-IAP1, it causes tumor cells to undergo apoptosis and enhances tumor necrosis factor (TNF-α)-induced apoptosis. [1] [3] The growth of xenografts made of four different tumor cell lines (B16 melanoma, MDA-435 breast cancer, TSU bladder cancer, and MGC80-3 gastric carcinoma) is inhibited by triptolide treatment for two to three weeks, demonstrating that TPL has a wide range of activity against tumors that contain both wild-type and mutant forms of p53.
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| Cell Assay |
The survival of differentiated PC12 cells given various doses of triptolide. Differentiated PC12 cells are cultured on 96-well plates with RPMI 1640 medium for stabilization before being exposed to Triptolide at various concentrations (0.01, 0.1, and 1 nM) for 24 hours. The study's concentrations have been selected. Next, the MTT assay is used to determine cell viability. Three times each condition and experiment are performed[3].
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| Animal Protocol |
Mice: Male BALB/C mice weighing 18 to 22 g are employed. The following four groups of mice (n=5 in each) were used to collect blood and tissue samples for the triptolide (TP) plasma kinetic study and toxicological assessment: (1) the normal+saline group; (2) the 1.0 mg/kg Triptolide+15 nmol negative control (NC) siRNA-siRNA group; (3) the 1.0 mg/kg Triptolide+15 nmol mdr1a-siRNA group; and (4) the 1.0 mg/kg Triptolide+10 mg/kg Tariquidar group. Triptolide and the inhibitor are given intravenously to mice to prevent complications brought on by drug absorption or a potential intestinal first-pass effect. Two days prior to the dose of triptolide, the siRNA group receives an intravenous injection of NC-siRNA or mdr1a-siRNA. For the mice in the triptolide+tariquidar group, a dose of intravenous tariquidar is administered 20 minutes before the triptolide injection. At 2, 5, 10, 15, 30, 60, and 120 minutes following the administration of Triptolide, blood samples are taken. Another group of mice were given Triptolide, and liver tissue samples were taken at 5, 30, 60, and 120 minutes later to determine the liver exposure. Three Triptolide groups, including Triptolide+NC-siRNA, Triptolide+mdr1a-siRNA, and Triptolide+Tariquidar, are planned for this experiment. Weighing the liver tissue samples is followed by homogenizing them in 10 volumes (w:v) of ice-cold saline. A tested LC-MS/MS technique is used to determine the levels of triptolide in plasma and liver tissue.
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| References |
| Molecular Formula |
C20H24O6
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| Molecular Weight |
360.41
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| Exact Mass |
360.16
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| Elemental Analysis |
C, 66.65; H, 6.71; O, 26.64
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| CAS # |
38748-32-2
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| Related CAS # |
Triptolide-d3
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| Appearance |
white solid powder
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| SMILES |
CC(C)[C@@]12[C@@H](O1)[C@H]3[C@@]4(O3)[C@]5(CCC6=C([C@@H]5C[C@H]7[C@]4([C@@H]2O)O7)COC6=O)C
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| InChi Key |
DFBIRQPKNDILPW-CIVMWXNOSA-N
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| InChi Code |
InChI=1S/C20H24O6/c1-8(2)18-13(25-18)14-20(26-14)17(3)5-4-9-10(7-23-15(9)21)11(17)6-12-19(20,24-12)16(18)22/h8,11-14,16,22H,4-7H2,1-3H3/t11-,12-,13-,14-,16+,17-,18-,19+,20+/m0/s1
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| Chemical Name |
(1S,2S,4S,5S,7R,8R,9S,11S,13S)-8-hydroxy-1-methyl-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-en-17-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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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: ≥ 1.17 mg/mL (3.25 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 11.7 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. Solubility in Formulation 2: ≥ 1.17 mg/mL (3.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 11.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2% DMSO+30% PEG 300+2% Tween 80+ddH2O: 3mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL | |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05166616 | Recruiting | Procedure: Biopsy Drug: Triptolide Analog |
Stage III Lung Cancer AJCC v8 Stage IV Lung Cancer AJCC v8 |
City of Hope Medical Center | March 7, 2022 | Phase 1 |
| NCT03403569 | Completed | Drug: Triptolide Wilfordii Drug: Placebo Oral Tablet |
HIV-infection/AIDS | Peking Union Medical College Hospital |
September 1, 2018 | Phase 3 |
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