| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Microtubules. Taccalonolide C is an antineoplastic agent that exerts its effects by binding to microtubules. Unlike other microtubule-targeting agents such as taxanes or vinca alkaloids, taccalonolides bind to a distinct site on tubulin and stabilize microtubules, leading to cell cycle arrest and apoptosis. This unique binding site makes taccalonolide C valuable for studying microtubule dynamics and for potentially overcoming resistance to other microtubule-targeting drugs. Its mechanism involves the stabilization of microtubules, preventing their depolymerization.
|
|---|---|
| ln Vitro |
In vitro, Taccalonolide C demonstrates potent antiproliferative activity against various cancer cell lines. It induces cell cycle arrest in the G2/M phase and promotes apoptosis. Its activity is attributed to its ability to stabilize microtubules, similar to paclitaxel, but with a distinct binding site. It is effective in cells that are resistant to paclitaxel, suggesting a unique mechanism of action. The compound's potency is measured using standard cytotoxicity assays such as MTT or SRB. It is a valuable tool for studying microtubule biology and drug resistance.
|
| ln Vivo |
In vivo activity data for Taccalonolide C are limited, but it is considered a valuable lead compound in anticancer drug development. As a natural product with potent in vitro activity, it has potential for in vivo efficacy in animal models of cancer. However, specific in vivo studies, including animal model efficacy, pharmacokinetics, or toxicity, are not detailed in the available literature. Its development is likely limited by its complex structure and potential for poor bioavailability. Further investigation is required.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Taccalonolide C focus on its interaction with tubulin. Typically, purified tubulin is incubated with the compound, and the extent of microtubule polymerization is measured spectrophotometrically (turbidity assay). The binding affinity can be assessed by competition assays with radiolabeled paclitaxel or other microtubule-binding agents. These cell-free assays confirm its mechanism as a microtubule stabilizer.
|
| Cell Assay |
In vitro cell-based assays for Taccalonolide C are performed in various cancer cell lines. Cells are treated with varying concentrations of the compound for defined periods (e.g., 48-72 hours). Cell viability is assessed using MTT or CellTiter-Glo assays. Cell cycle analysis is performed using propidium iodide (PI) staining and flow cytometry to measure G2/M arrest. Apoptosis is assessed by Annexin V/PI staining. The effects on microtubule organization are visualized by immunofluorescence staining of tubulin. These assays characterize its antiproliferative and mechanistic properties.
|
| Animal Protocol |
Specific in vivo animal experimental protocols for Taccalonolide C are not described in the available literature. As a natural product lead compound, it may be evaluated in mouse xenograft models of cancer. Tumor-bearing mice would be administered Taccalonolide C, and tumor growth inhibition would be monitored. However, no such studies are reported in the available sources. Its in vivo development is likely in early stages.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Taccalonolide C are not reported in the available literature. As a complex natural product with high molecular weight (702.74) and multiple polar groups, it is expected to have poor oral bioavailability. Its solubility, half-life, and metabolism are unknown. It is typically handled as a solid and stored desiccated at -20°C. Its PK profile would be a significant challenge for drug development.
|
| Toxicity/Toxicokinetics |
Toxicological data for Taccalonolide C are not detailed in the available literature. It is a research compound with potent antimitotic activity, suggesting significant cytotoxicity. No LD50 values or repeated-dose toxicity studies have been reported. Standard safety pharmacology studies have not been performed. As with all research chemicals, appropriate safety precautions should be taken when handling. Its specific toxicity profile has not been established.
|
| References | |
| Additional Infomation |
Reports have indicated that plants in the genus Konjac contain konjac lactone C, and relevant data are available for reference.
Taccalonolide C is a highly oxygenated pentacyclic steroidal compound isolated from Tacca plants. It is an anti-cancer agent and a valuable lead compound in anticancer drug development. Its molecular formula is C36H46O14, and its molecular weight is 702.74. It is also known as root tuber ketone lactone C. It binds to microtubules at a distinct site, making it useful for studying microtubule dynamics and drug resistance. It is available for research use only. |
| Molecular Formula |
C36H46O14
|
|---|---|
| Molecular Weight |
272.73282
|
| Exact Mass |
702.288
|
| CAS # |
117803-96-0
|
| PubChem CID |
132076228
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
50
|
| Complexity |
1610
|
| Defined Atom Stereocenter Count |
18
|
| SMILES |
C[C@@H]1CC(=O)[C@]2([C@H]3[C@H]1[C@@]4([C@@H]([C@H]3OC(=O)[C@@]2(C)O)[C@H]5[C@H]([C@@H]([C@@H]4OC(=O)C)OC(=O)C)[C@@]6([C@H](C[C@H]7[C@@H]([C@@H]6OC(=O)C)O7)C(=O)[C@@H]5OC(=O)C)C)C)C
|
| InChi Key |
RXQVUONAHNHYNF-XSUQWDDVSA-N
|
| InChi Code |
InChI=1S/C36H46O14/c1-12-10-19(41)35(8)24-21(12)34(7)22(28(24)50-32(43)36(35,9)44)20-23(29(46-14(3)38)31(34)48-16(5)40)33(6)17(25(42)27(20)45-13(2)37)11-18-26(49-18)30(33)47-15(4)39/h12,17-18,20-24,26-31,44H,10-11H2,1-9H3/t12-,17-,18+,20+,21+,22-,23-,24+,26+,27-,28-,29+,30+,31+,33+,34-,35+,36-/m1/s1
|
| Chemical Name |
[(1R,2S,3S,4R,6S,8S,10S,11R,12R,13S,14S,15R,16R,17S,18R,21S,22S,25R)-4,11,15-triacetyloxy-22-hydroxy-12,16,18,21,22-pentamethyl-5,20,23-trioxo-9,24-dioxaheptacyclo[15.7.1.02,16.03,13.06,12.08,10.021,25]pentacosan-14-yl] acetate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~142.30 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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: ≥ 2.5 mg/mL (3.56 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 and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6666 mL | 18.3332 mL | 36.6663 mL | |
| 5 mM | 0.7333 mL | 3.6666 mL | 7.3333 mL | |
| 10 mM | 0.3667 mL | 1.8333 mL | 3.6666 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
