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| 25mg |
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Triptonide (NSC-165677; PG-492), a natural product isolated from Tripterygium wilfordii Hook, a novel and potent Wnt/β-catenin inhibitor that inhibited the proliferation of mouse splenocytes induced by suboptimal concentration of concanavalin A or lipopolysaccharide at concentrations of 0.02, 0.1, and 0.5 mg/ml. Triptonide can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. It also effectively induced apoptosis of Wnt-dependent cancer cells, supporting the therapeutic potential of triptonide.
| ln Vitro |
Triptonide stimulates Wnt-dependent cancer cell apoptosis and inhibits Wnt/β-catenin signaling via the β-catenin C-terminal transactivation domain [1]. Triptonide, with an IC50 of 5.7 nM and 4.8 nM, respectively, potently suppresses the growth of human B lymphoma Raji and T lymphoma Jurkat cells [2]. The capacity of B lymphoma cells to form colonies is considerably inhibited by triptolide (2.5-10 nM; 6 days) [2]. Repunide (20 nM; 3 days) decreases BCL2 protein levels in lymphoma cells while increasing apoptosis by activating PARP and caspase 3 [2]. Significant reductions in total and phosphorylated Lyn protein, as well as in Lyn downstream ERK and ATK signaling pathways, are observed with triptolide (5-10 nM; 72 hours) [2].
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| ln Vivo |
Mice treated with 5 mg/kg of rapunide intraperitoneally once a day for 34 days show significant anti-lymphoma effects [2].
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| Cell Assay |
Cell proliferation assay [2]
Cell Types: B lymphoma Raji cells, T lymphoma Jurkat cells Tested Concentrations: 0-80 nM Incubation Duration: 3 days, 6 days Experimental Results: Inhibited the tumorigenic ability of lymphoma cells in a dose-dependent manner. Apoptosis analysis [2] Cell Types: Raji cells Tested Concentrations: 5 nM, 10 nM, 20 nM Incubation Duration: 3 days Experimental Results: No significant induction of apoptosis under effective tumor growth inhibition (2.5-10 nM); Moderately induces apoptosis in lymphoma cells (20 nM). Western Blot Analysis[2] Cell Types: Raji Cell Tested Concentrations: 5 nM, 10 nM, 20 nM Incubation Duration: 3 days Experimental Results: Proapoptotic proteins PARP and caspase 3 (5-10 nM) in lymphoma cells are not strongly activated ; Dramatically activates PARP and caspase 3 (20 nM); Dramatically reduces anti-apoptotic BCL2 levels. RT-PCR[2] Cell Types: Raji cells Tested Concentrations: 5 nM, 10 nM Incubation Duration: 72 hrs (hours) Experimental Results: Lyn mRNA levels were Dramatically diminished in lymphoma cells. |
| Animal Protocol |
Animal/Disease Models: Eightweeks old female NOD/SCID (severe combined immunodeficient) mouse (18-22 g) with 3 x 107 Raji cell xenografts [2]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection daily for 34 Experimental Results: Effectively inhibit the growth and tumorigenic ability of lymphoma cells. |
| References |
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| Additional Infomation |
Triptonide is a diterpene triepoxide that is triptobenzene K in which the acylhydroquinone moiety has undergone oxidation to the corresponding triepoxyketone derivative. It has been isolated from the roots of Tripterygium wilfordii. It has a role as an antineoplastic agent, an anti-inflammatory agent and an immunosuppressive agent. It is a cyclic ketone, an organic heteroheptacyclic compound, a diterpene triepoxide and a butenolide.
Triptonide has been reported in Tripterygium wilfordii and Tripterygium hypoglaucum with data available. |
| Molecular Formula |
C20H22O6
|
|---|---|
| Molecular Weight |
358.3851
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| Exact Mass |
358.141
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| CAS # |
38647-11-9
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| PubChem CID |
65411
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
581.1±50.0 °C at 760 mmHg
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| Flash Point |
257.8±30.2 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.638
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| LogP |
1.49
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
|
| Heavy Atom Count |
26
|
| Complexity |
860
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| Defined Atom Stereocenter Count |
8
|
| 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(C2=O)O7)COC6=O)C
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| InChi Key |
SWOVVKGLGOOUKI-ZHGGVEMFSA-N
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| InChi Code |
InChI=1S/C20H22O6/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/h8,11-14H,4-7H2,1-3H3/t11-,12-,13-,14-,17-,18-,19+,20+/m0/s1
|
| Chemical Name |
(5bS,6aS,7aS,8aS,9aS,9bS,10aS,10bS)-8a-isopropyl-10b-methyl-2,5,5b,6,6a,9a,9b,10b-octahydrotris(oxireno)[2',3':4b,5;2'',3'':6,7;2''',3''':8a,9]phenanthro[1,2-c]furan-3,8(1H,8aH)-dione
|
| Synonyms |
NSC165677; PG492; NSC-165677; PG-492; NSC 165677; PG 492;
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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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~279.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.98 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 25.0 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: ≥ 2.5 mg/mL (6.98 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7903 mL | 13.9513 mL | 27.9026 mL | |
| 5 mM | 0.5581 mL | 2.7903 mL | 5.5805 mL | |
| 10 mM | 0.2790 mL | 1.3951 mL | 2.7903 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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