| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Cucurbitacin C targets several cellular signaling pathways, including the STAT3, NF-κB, and MAPK pathways, to cause cell cycle arrest and death in cancer cells. It substantially suppresses Akt signaling by preventing Akt phosphorylation at Ser473. The PI3K-Akt signaling pathway is one of the main pathways implicated in its cell growth arrest and apoptosis-inducing effects.
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|---|---|
| ln Vitro |
In vitro, Cucurbitacin C decreases the proliferation and clonogenic potential of various cancer cells in a dose-dependent manner. In many cancer lines, low-dose treatment results in cell cycle arrest in the G1/M or G2/A stages, while high-dose treatment leads to cancer cell death. It has been shown to suppress the growth of cholangiocarcinoma cells.
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| ln Vivo |
In vivo, Cucurbitacin C treatment (0.1 mg/kg body weight) significantly increased apoptosis and successfully reduced the formation of xenograft tumors formed from cancer cells in athymic nude mice. These results demonstrate that Cucurbitacin C has therapeutic promise against human tumors.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols for Cucurbitacin C typically involve assessing its effects on cell signaling pathways. For example, Western blot analysis is used to measure the phosphorylation status of proteins like Akt (Ser473) to confirm target engagement. Cell proliferation assays (e.g., MTT) and clonogenic assays are used to assess its antiproliferative effects.
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| Cell Assay |
In vitro cell-based assay protocols for Cucurbitacin C involve treating various cancer cell lines with the compound. Cells are seeded in multi-well plates, treated with varying concentrations, and then assessed for proliferation, cell cycle distribution (by flow cytometry), and apoptosis (by Annexin V staining). Signaling pathway modulation is confirmed by Western blot.
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| Animal Protocol |
In vivo animal experimental protocols for Cucurbitacin C have been established in xenograft models. Cancer cells are implanted subcutaneously in athymic nude mice. Once tumors are established, mice are treated with Cucurbitacin C (e.g., 0.1 mg/kg). Tumor growth is monitored, and at the end of the study, tumors are excised for analysis of apoptosis and signaling pathways.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cucurbitacin C have not been extensively characterized in published studies. Specific PK parameters such as half-life, Cmax, and AUC have not been reported. As a triterpenoid, it would be expected to have low oral bioavailability.
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| Toxicity/Toxicokinetics |
Toxicological data for Cucurbitacin C are limited. As a member of the cucurbitacin family, which are known to be highly toxic, it should be handled with extreme caution. Standard laboratory safety precautions are essential.
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| References | |
| Additional Infomation |
Cucurbitacin C is a cucurbitacin. It has been reported to exist in Gentiana alba, Cucumis sativus, and other organisms with relevant data. Mechanism of Action: This study investigated the binding of cucurbitacin to glucocorticoid receptors in cell-free HeLa cells and intact cells by competing with (3)H-cortisol. Cucurbitacin reduced (3)H-cortisol binding. The difference in binding affinity at the two temperatures suggests that cucurbitacin is metabolized under physiological conditions. A linear correlation was observed between the logarithm of the relative binding affinity of cucurbitacin and the logarithm of its cytotoxic activity. Therefore, the binding of cucurbitacin to glucocorticoid receptors appears to be a necessary step for these compounds to exert their cytotoxic effects.
Cucurbitacin C is a research-grade compound with demonstrated anticancer activity in preclinical models. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves inhibition of the STAT3, NF-κB, MAPK, and PI3K-Akt signaling pathways. The compound is available exclusively for research purposes. |
| Molecular Formula |
C32H48O8
|
|---|---|
| Molecular Weight |
560.72
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| Exact Mass |
560.335
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| CAS # |
5988-76-1
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| PubChem CID |
5281317
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| Appearance |
NEEDLES FROM ETHYL ACETATE
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| Density |
1.23g/cm3
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| Boiling Point |
701ºC at 760 mmHg
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| Melting Point |
207-207.5 °C
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| Flash Point |
218.6ºC
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| Index of Refraction |
1.574
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| LogP |
3.292
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
40
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
9
|
| SMILES |
CC(=O)OC(C)(C)/C=C/C(=O)[C@@](C)([C@H]1[C@@H](C[C@@]2([C@@]1(CC(=O)[C@@]3([C@H]2CC=C4[C@H]3CC[C@@H](C4(C)C)O)CO)C)C)O)O
|
| InChi Key |
DGIGXLXLGBAJJN-TUOUHCSQSA-N
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| InChi Code |
InChI=1S/C32H48O8/c1-18(34)40-27(2,3)14-13-24(37)31(8,39)26-21(35)15-29(6)22-11-9-19-20(10-12-23(36)28(19,4)5)32(22,17-33)25(38)16-30(26,29)7/h9,13-14,20-23,26,33,35-36,39H,10-12,15-17H2,1-8H3/b14-13+/t20-,21-,22+,23+,26+,29+,30-,31+,32+/m1/s1
|
| Chemical Name |
[(E,6R)-6-[(3S,8S,9R,10R,13R,14S,16R,17R)-3,16-dihydroxy-9-(hydroxymethyl)-4,4,13,14-tetramethyl-11-oxo-1,2,3,7,8,10,12,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl]-6-hydroxy-2-methyl-5-oxohept-3-en-2-yl] acetate
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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)
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| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7834 mL | 8.9171 mL | 17.8342 mL | |
| 5 mM | 0.3567 mL | 1.7834 mL | 3.5668 mL | |
| 10 mM | 0.1783 mL | 0.8917 mL | 1.7834 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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