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Triptolide (Synonyms: NSC 163062, PG 490)

Catalog No.GC14402 Copy One-Click Copy Product Info

Triptolide is a diterpene triepoxide isolated for the first time from the medicinal plant Tripterygium wilfordii, exhibiting immunosuppressive, anti-inflammatory, anti-proliferative, and antitumor effects.

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Triptolide Chemical Structure

Cas No.: 38748-32-2

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10mM (in 1mL DMSO)
$77.00
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5mg
$54.00
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10mg
$89.00
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25mg
$185.00
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1g
$1,258.00
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Sample solution is provided at 25 µL, 10mM.



Description of Triptolide

Triptolide is a diterpene triepoxide isolated for the first time from the medicinal plant Tripterygium wilfordii, exhibiting immunosuppressive, anti-inflammatory, anti-proliferative, and antitumor effects. It acts as an inhibitor of NF-κB activation, where NF-κB is a family of transcription factor protein complexes[1]. Triptolide possesses broad-spectrum anticancer activity, inhibiting the development of colon cancer, breast cancer, renal cell carcinoma, and cervical cancer[2].

In vitro, triptolide (50 nM, 72 h) significantly inhibits the proliferation of ovarian cancer cells SKOV3 and A2780. Triptolide (15 nM, 48h) significantly inhibits cell migration and blocks the invasive capability of cells[2]. Triptolide (50-200 nmol/L) incubated with PANC-1 and MiaPaCa-2 cells significantly reduces cell viability without affecting the viability of normal pancreatic ductal cells[3]. The IC50 value of triptolide on RSF cell viability is 74.3 nM, and its IC50 value on RSF cell proliferation is 20.4 nM[4]. Triptolide (0-150 nM) significantly inhibits the viability of HK1, FaDu, and C666-1 cells in a dose- and time-dependent manner[5].

In vivo, treatment with triptolide (1 mg/kg/d, p.o.) for three weeks in nude mice reduced the number of metastatic nodules by approximately 80%[2]. Triptolide (0.2 mg/kg/d) administered to mice with transplanted pancreatic tumors for 60 days reduced pancreatic cancer growth and significantly decreased local tumor spread[3].

References:
[1] Zhang W, et al. Triptolide Combined with Radiotherapy for the Treatment of Nasopharyngeal Carcinoma via NF-κB-Related Mechanism. Int J Mol Sci. 2016 Dec 19;17(12).
[2] Zhao H, Yang Z, Wang X, et al. Triptolide inhibits ovarian cancer cell invasion by repression of matrix metalloproteinase 7 and 19 and upregulation of E-cadherin[J]. Experimental & molecular medicine, 2012, 44(11): 633-641.
[3] Phillips P A , Dudeja V , Mccarroll J A ,et al.Triptolide Induces Pancreatic Cancer Cell Death via Inhibition of Heat Shock Protein 70[J].Cancer Research, 2007, 67(19):9407.
[4] Kusunoki N, Yamazaki R, Kitasato H, Beppu M, Aoki H, Kawai S: Triptolide, an active compound identified in a traditional Chinese herb, induces apoptosis of rheumatoid synovial fibroblasts. BMC Pharmacol 2004, 4:2.
[5] Cai J, et al. Natural product triptolide induces GSDME-mediated pyroptosis in head and neck cancer through suppressing mitochondrial hexokinase-ΙΙ. J Exp Clin Cancer Res. 2021;40(1):190. Published 2021 Jun 9.

Protocol of Triptolide

Cell experiment [1]:

Cell lines

SKOV3 and A2780 cells

Preparation Method

SKOV3 and A2780 cells were plated in 96-well plates (5 × 103/well). 24h later, triptolide was added to a final concentration of 0, 1.5, 5, 15, 50, or 150 nM for 72 h.

Reaction Conditions

0, 1.5, 5, 15, 50, or 150 nM; 72 h

Applications

Triptolide (50nM, 72 h) noticeably inhibited ovarian cancer cell proliferation. Triptolide (15nM) significantly inhibited cell migration 48h after wounding. Triptolide (15nM) markedly blocked the invasive capacity of SKOV3 and A2780 cells.

Animal experiment [2]:

Animal models

orthotopic mouse model

Preparation Method

Mice were then randomized into two treatment groups: (a) control and (b) triptolide-treated mice. Mice were given daily i.p. injections of triptolide (0.2 mg/kg) or vehicle (DMSO) for 60 days.

Dosage form

0.2 mg/kg/d; 60 days; i.p.

Applications

After a daily injection of triptolide (0.2 mg/kg) for 60 days, the tumor volume was significantly reduced. triptolide also significantly reduced the incidence of local-regional tumor spread.

References:

[1] Zhao H, Yang Z, Wang X, et al. Triptolide inhibits ovarian cancer cell invasion by repression of matrix metalloproteinase 7 and 19 and upregulation of E-cadherin[J]. Experimental & molecular medicine, 2012, 44(11): 633-641.
[2] Phillips P A , Dudeja V , Mccarroll J A ,et al. Triptolide Induces Pancreatic Cancer Cell Death via Inhibition of Heat Shock Protein 70[J].Cancer Research, 2007, 67(19):9407.

Chemical Properties of Triptolide

Cas No. 38748-32-2 SDF
Synonyms NSC 163062, PG 490
Chemical Name (6aS,7aS,8R,8aR,9aS,9bS,10aS,10bS)-8-hydroxy-8a-isopropyl-10b-methyl-1,5,5b,6,6a,8,8a,9a,9b,10b-decahydrotris(oxireno)[2',3':4b,5;2'',3'':6,7;2''',3''':8a,9]phenanthro[1,2-c]furan-3(2H)-one
Canonical SMILES CC(C)C12C(O1)C3C4(O3)C5(CCC6=C(C5CC7C4(C2O)O7)COC6=O)C
Formula C20H24O6 M.Wt 360.41
Solubility ≥ 36 mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Triptolide

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.7746 mL 13.8731 mL 27.7462 mL
5 mM 554.9 μL 2.7746 mL 5.5492 mL
10 mM 277.5 μL 1.3873 mL 2.7746 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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