| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Silvestrol aglycone (enantiomer) targets eukaryotic initiation factor 4A (eIF4A), an RNA helicase essential for cap-dependent mRNA translation initiation. By inhibiting eIF4A, it blocks cap-dependent mRNA translation, suppressing the expression of oncogenic and survival-related proteins. This leads to antiproliferative and pro-apoptotic effects.
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|---|---|
| ln Vitro |
In vitro, Silvestrol aglycone (enantiomer) exhibits potent antiproliferative and pro-apoptotic activity against cancer cell lines. Its unique mechanism of eIF4A inhibition makes it a valuable tool for studying translation regulation in cancer. Detailed IC50 values against specific cell lines are not extensively reported.
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| ln Vivo |
In vivo, Silvestrol aglycone (enantiomer) demonstrates strong anticancer activity in preclinical studies, particularly against hematologic malignancies and solid tumors. Its unique mechanism makes it a valuable tool for cancer research and therapeutic development.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Silvestrol aglycone (enantiomer) are performed using purified eIF4A protein or eIF4F complex components. The compound is incubated with eIF4A, ATP, and RNA substrates. eIF4A helicase activity is measured using fluorescence-based or gel-based unwinding assays. Binding affinity is determined by surface plasmon resonance or isothermal titration calorimetry.
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| Cell Assay |
Cellular assays for Silvestrol aglycone (enantiomer) are conducted using cancer cell lines from hematologic malignancies and solid tumors. Cells are treated with serial dilutions of the compound (0.1 nM to 10 uM) for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo assays. Cap-dependent translation is evaluated by reporter gene assays or polysome profiling. Apoptosis is measured by Annexin V/PI staining and caspase activation.
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| Animal Protocol |
In vivo efficacy studies for Silvestrol aglycone (enantiomer) are conducted in xenograft mouse models bearing human tumor xenografts. The compound is administered via intraperitoneal or oral routes at doses determined from pharmacokinetic studies. Tumor volume is measured, and TGI is calculated. Pharmacodynamic markers including eIF4A target engagement and translation inhibition are assessed in tumor tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Silvestrol aglycone (enantiomer) have not been extensively characterized. The compound has a molecular weight of 478.49 and formula C27H26O8. It is a solid powder and is typically stored at -20degC. Bioavailability and half-life data are not available in the literature.
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| Toxicity/Toxicokinetics |
Toxicological data for Silvestrol aglycone (enantiomer) are limited. As a potent translation inhibitor, standard safety assessments would include evaluation of cytotoxicity in normal cells to assess therapeutic index. No significant toxicity has been reported in the available literature. The compound is for research use only.
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| References | |
| Additional Infomation |
Silvestrol aglycone (enantiomer) is a research-use compound not approved for clinical therapeutic applications. It is a valuable tool for studying eIF4A-mediated translation regulation, cap-dependent mRNA translation, and the development of anticancer agents targeting the translation initiation complex. The compound is for research use only and not for human therapeutic application.
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| Molecular Formula |
C27H26O8
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|---|---|
| Molecular Weight |
478.4905
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| Exact Mass |
478.162
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| CAS # |
1112993-18-6
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| Related CAS # |
Silvestrol aglycone;960365-65-5
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| PubChem CID |
124670983
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
762
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| Defined Atom Stereocenter Count |
5
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| SMILES |
COC1=CC=C(C=C1)[C@@]23[C@H]([C@@H]([C@@H]([C@@]2(C4=C(O3)C=C(C=C4OC)O)O)O)C(=O)OC)C5=CC=CC=C5
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| InChi Key |
HYLOONIBWUNKDH-DSVANHEQSA-N
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| InChi Code |
InChI=1S/C27H26O8/c1-32-18-11-9-16(10-12-18)27-22(15-7-5-4-6-8-15)21(25(30)34-3)24(29)26(27,31)23-19(33-2)13-17(28)14-20(23)35-27/h4-14,21-22,24,28-29,31H,1-3H3/t21-,22-,24-,26+,27+/m0/s1
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| Chemical Name |
methyl (1S,2S,3R,3aS,8bR)-1,6,8b-trihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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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) |
DMSO : ≥ 114 mg/mL (~238.25 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (15.67 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 75.0 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: ≥ 7.5 mg/mL (15.67 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 75.0 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: ≥ 7.5 mg/mL (15.67 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 | 2.0899 mL | 10.4495 mL | 20.8991 mL | |
| 5 mM | 0.4180 mL | 2.0899 mL | 4.1798 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0899 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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