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| Targets |
Telekin targets the mitochondrial apoptosis pathway. It activates mitochondria-mediated apoptosis, leading to cancer cell death. The compound's sesquiterpene lactone structure contains an α-methylene-γ-lactone moiety, which is a known pharmacophore for covalent modification of nucleophilic groups (such as thiols) in proteins, potentially affecting various signaling pathways. By activating the mitochondrial apoptosis pathway, Telekin induces the release of cytochrome c and other pro-apoptotic factors from mitochondria, leading to caspase activation and programmed cell death. This mechanism underlies its anti-cancer activity.
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| ln Vitro |
In vitro, Telekin has demonstrated anti-cancer activity by activating mitochondria-mediated apoptosis in cancer cells. The compound induces cell death through the mitochondrial pathway, leading to caspase activation and apoptosis. However, specific in vitro data such as IC50 values, cell lines tested, and detailed mechanism studies are not extensively documented in the available literature. The compound's sesquiterpene lactone structure suggests it may have additional activities, including anti-inflammatory and antimicrobial effects. Researchers should consult primary literature for detailed in vitro characterization.
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| ln Vivo |
In vivo studies with Telekin are limited in publicly available literature. The compound's anti-cancer activity observed in vitro suggests potential for in vivo antitumor efficacy, but specific animal studies (xenograft models, dosing regimens, tumor growth inhibition) have not been extensively reported. The compound's natural product origin and sesquiterpene lactone structure suggest it may have pharmacokinetic and toxicity profiles typical of this class of compounds. Researchers interested in in vivo applications should consult the primary literature for updated information and conduct appropriate studies to determine effective dosing and administration routes.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Telekin are not extensively documented. As a sesquiterpene lactone, the compound may interact with various cellular targets through covalent modification of nucleophilic groups. The compound's effects on mitochondrial apoptosis can be assessed by measuring mitochondrial membrane potential (using fluorescent dyes such as JC-1), cytochrome c release (by Western blot or ELISA), caspase activation (by fluorogenic substrates), and apoptosis (by Annexin V/PI staining). These assays would be used to characterize the compound's mechanism of action. However, specific detailed protocols are not well-documented in the available literature.
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| Cell Assay |
Cell-based assays for Telekin would focus on its anti-cancer activity and induction of apoptosis. Cancer cell lines would be treated with Telekin at various concentrations, and cell viability would be assessed using MTT, CCK-8, or CellTiter-Glo assays. Apoptosis would be assessed by Annexin V/PI staining, caspase activity assays, and Western blot for PARP cleavage and caspase activation. Mitochondrial membrane potential would be measured using fluorescent dyes such as JC-1. However, specific detailed protocols for Telekin are not extensively documented in the available literature. Researchers should develop appropriate cell-based assays based on the compound's reported mechanism of action.
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| Animal Protocol |
In vivo animal protocols for Telekin are not documented in publicly available literature. Based on the compound's anti-cancer activity, typical study designs would involve administration of Telekin in rodent xenograft models bearing human tumor cells. Doses would be determined from in vitro potency data and preliminary toxicity assessments. Route of administration would depend on the compound's solubility and bioavailability. Endpoints would include tumor growth inhibition, survival, histopathological analysis of tumors, and assessment of apoptosis in tumor tissues. Researchers should consult primary literature and conduct appropriate studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Telekin have not been extensively characterized. The compound has molecular weight 248.32 and molecular formula C15H20O3. It is soluble in DMSO (~27.5 mg/mL, ~110.74 mM). LogP is 2.1. Specific pharmacokinetic parameters such as half-life, Cmax, AUC, bioavailability, and tissue distribution have not been reported. Storage: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month. Researchers planning in vivo studies should conduct appropriate pharmacokinetic characterization.
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| Toxicity/Toxicokinetics |
Toxicology data for Telekin are limited in publicly available sources. As a natural product sesquiterpene lactone, the compound may have potential toxicities at high doses, including hepatotoxicity, nephrotoxicity, or gastrointestinal effects, which are common for this class of compounds. However, specific toxicology studies have not been reported. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling Telekin. The compound should be stored properly and disposed of in accordance with applicable regulations. Researchers should consult the material safety data sheet (MSDS) for detailed safety information.
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| References | |
| Additional Infomation |
Telekin is a sesquiterpene lactone. It has been reported to exist in Inula grandis, Carpesium macrocephalum, and other organisms with relevant data.
Telekin has CAS number 6752-90-5, molecular formula C15H20O3, and molecular weight 248.32. It is a eucalyptus-type sesquiterpene lactone compound extracted from Carpesium divaricatum. Telekin can activate mitochondria-mediated apoptosis and has anti-cancer activity. Synonyms: 特勒内酯 (Chinese). Purity: ≥98%. LogP: 2.1. Solubility: DMSO ~27.5 mg/mL (~110.74 mM). Storage: powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month. Not approved for clinical use; for research purposes only. The compound is a valuable tool for studying mitochondrial apoptosis and developing anti-cancer therapeutics. |
| Molecular Formula |
C15H20O3
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|---|---|
| Molecular Weight |
248.317
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| Exact Mass |
248.141
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| CAS # |
6752-90-5
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| Related CAS # |
6752-90-5
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| PubChem CID |
12443309
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
453
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@]12CCCC(=C)[C@@]1(C[C@H]3[C@@H](C2)OC(=O)C3=C)O
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| InChi Key |
LIDPBIULZNRIJE-QHSBEEBCSA-N
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| InChi Code |
InChI=1S/C15H20O3/c1-9-5-4-6-14(3)8-12-11(7-15(9,14)17)10(2)13(16)18-12/h11-12,17H,1-2,4-8H2,3H3/t11-,12-,14-,15-/m1/s1
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| Chemical Name |
(3aR,4aR,8aR,9aR)-4a-hydroxy-8a-methyl-3,5-dimethylidene-4,6,7,8,9,9a-hexahydro-3aH-benzo[f][1]benzofuran-2-one
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| Synonyms |
Telekin
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.0271 mL | 20.1353 mL | 40.2706 mL | |
| 5 mM | 0.8054 mL | 4.0271 mL | 8.0541 mL | |
| 10 mM | 0.4027 mL | 2.0135 mL | 4.0271 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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