| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Minnelide targets multiple signaling pathways involved in cancer cell growth and survival. As a prodrug of triptolide, its active moiety is believed to target TAK1 (TGF-β-activated kinase 1). It induces and promotes apoptosis in cancer cells. It has demonstrated efficacy against various cancer types in preclinical models.
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| ln Vitro |
Following treatment in the presence (but not in the absence) of phosphatase, pancreatic cancer cell lines treated with methylide (0-200 nM; 48 hours) demonstrated a significant reduction in cell viability [2].
In vitro, minnelide has shown potent anticancer activity in various cancer cell lines. It induces apoptosis and has been shown to be effective against both CD133(-) and CD133(+) populations in tumors. Its activity has been demonstrated in pancreatic cancer and other tumor types. |
| ln Vivo |
Minnelide (intraperitoneal injection; 0.1-0.6 mg/kg; once daily or twice daily) results in significant decreases in tumor weight and volume at the conclusion of treatment and increases survival in an orthotopic model of MIA PaCa-2-derived human pancreatic cancer incidence of pancreatic tumors [2]. Minnelide (ip; 0.42 mg/kg; once daily; 28 days) limits local spread of metastatic S2-013 cells and resulting in a decrease in mean tumor weight in a pancreatic cancer xenograft model [2]. Minnelide (intraperitoneal injection; 0.42 mg/kg, 0.21 mg/kg; once daily) produced tumor regression, and in human pancreatic cancer xenografts from SCID mice, tumors from Minnelide-treated animals displayed fibrosis and consolidation. The existence of shrinking core [2].
In vivo, minnelide (injection intraperitoneally; 0.42 mg/kg; once daily; 28 days) prevents locoregional spread and leads to a decrease in average tumor weight in a xenograft model of pancreatic cancer with metastatic S2-013 cells. It is highly effective in reducing pancreatic tumor growth and spread, and improving survival. |
| Enzyme Assay |
The in vitro binding/activity assays for minnelide are related to its active moiety, triptolide. Its effects on TAK1 and other signaling pathways can be assessed using kinase assays or cell-based reporter assays. Its pro-apoptotic activity is assessed in cancer cell lines by measuring markers of apoptosis.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Pancreatic Cancer Cell Types: S2-013, MIA PaCa-2, S2-VP10 and Panc-1 Cell Tested Concentrations: 0.100 nM, 200 nM Incubation Duration: 48 hrs (hours) Experimental Results: Pancreatic Cancer Cell Lines diminished cell viability in vitro. In vitro cellular assays for minnelide assess its antiproliferative and pro-apoptotic effects. Cancer cell lines are treated with minnelide, and cell viability and apoptosis are measured. Its effects on both CD133(-) and CD133(+) populations have been demonstrated. These assays demonstrate the compound's potent anticancer activity in a relevant cellular context. |
| Animal Protocol |
Animal/Disease Models: Pancreatic cancer orthotopic model of MIA PaCa 2-derived human pancreatic tumors in athymic nude mice [2]
Doses: 0.1-0.6 mg/kg Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. 0.1-0.6 mg/kg; one time/day or twice (two times) daily Experimental Results: Prevents the growth of pancreatic tumors in the body. Animal/Disease Models: athymic nude mouse metastatic S2-013 cell line pancreatic cancer xenograft model [2] Doses: 0.42 mg/kg Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. 0.42 mg/kg; one time/day Experimental Results: Prevented widespread spread from the primary injection site. Animal/Disease Models: SCID mouse human pancreatic cancer xenograft [2] Doses: 0.21 mg/kg, 0.42 mg/kg Route of Administration: intraperitoneal (ip) injection; 0.42 mg/kg; one time/day Experimental Results: diminished human xenografts from patients tumor burden. In vivo animal studies for minnelide have been conducted in xenograft models of pancreatic cancer. Minnelide is administered intraperitoneally, and tumor growth, spread, and survival are assessed. These studies demonstrate the compound's in vivo efficacy against pancreatic cancer. |
| ADME/Pharmacokinetics |
Minnelide sodium is a water-soluble prodrug that is administered via injection. Its water solubility is a key feature that improves the bioavailability of triptolide. However, detailed pharmacokinetic parameters such as half-life are not extensively detailed in the available literature. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for minnelide are not extensively detailed in the available literature. As a prodrug of triptolide, its toxicity profile is likely related to the active moiety. However, its water solubility and targeted delivery may improve its safety profile compared to triptolide. It is intended for research purposes only.
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| References | |
| Additional Infomation |
Tripterygium wilfordii analogues are water-soluble compounds, analogues of the diterpenoid tricyclic oxide tripterpenoid, isolated from the traditional Chinese medicine Tripterygium wilfordii Hook.f., and possess potential antitumor activity. Upon intravenous injection, these analogues inhibit heat shock protein 70 (HSP70), thereby preventing HSP70-mediated inhibition of apoptosis. This leads to the induction of apoptosis and a reduction in cancer cell growth. HSP70 is a molecular chaperone highly expressed in various cancer cells, playing a crucial role in inhibiting caspase-dependent and caspase-independent apoptosis.
Minnelide sodium is a water-soluble prodrug of triptolide with potent antitumor activity, particularly in pancreatic cancer. It promotes apoptosis and has been shown to reduce tumor growth and improve survival in preclinical models. It is a research compound and is not approved for clinical use. |
| Molecular Formula |
C21H25NA2O10P
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|---|---|
| Molecular Weight |
514.3705
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| Exact Mass |
514.098
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| CAS # |
1254702-87-8
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| Related CAS # |
1254885-39-6 (free acid);1254702-87-8 (sodium);
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| PubChem CID |
46203139
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
9
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| SMILES |
P(=O)([O-])([O-])OC([H])([H])O[C@]1([H])[C@]2(C([H])(C([H])([H])[H])C([H])([H])[H])[C@]([H])([C@@]3([H])[C@]4([C@@]5(C([H])([H])[H])C([H])([H])C([H])([H])C6C(=O)OC([H])([H])C=6[C@]5([H])C([H])([H])[C@@]5([H])[C@]41O5)O3)O2.[Na+].[Na+]
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| InChi Key |
ZHBJMVNZRZUQEP-KIKMAQITSA-L
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| InChi Code |
InChI=1S/C21H27O10P.2Na/c1-9(2)19-14(30-19)15-21(31-15)18(3)5-4-10-11(7-26-16(10)22)12(18)6-13-20(21,29-13)17(19)27-8-28-32(23,24)25;;/h9,12-15,17H,4-8H2,1-3H3,(H2,23,24,25);;/q;2*+1/p-2/t12-,13-,14-,15-,17+,18-,19-,20+,21+;;/m0../s1
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| Chemical Name |
disodium;[(1S,2S,4S,5S,7S,8R,9R,11S,13S)-1-methyl-17-oxo-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-8-yl]oxymethyl phosphate
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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. |
| 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) |
H2O : ~93.33 mg/mL (~181.45 mM)
DMSO : ~16.67 mg/mL (~32.41 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 1.67 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 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9441 mL | 9.7206 mL | 19.4413 mL | |
| 5 mM | 0.3888 mL | 1.9441 mL | 3.8883 mL | |
| 10 mM | 0.1944 mL | 0.9721 mL | 1.9441 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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