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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Silvestrol aglycone targets the translation initiation machinery in cancer cells, specifically inhibiting protein synthesis by blocking the 5′ untranslated region (UTR)-mediated translation of oncogenes such as myc. It induces apoptosis through the mitochondrial/apoptosome pathway. The compound also causes disruption of the mitochondrial transmembrane potential and cytochrome c release.
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| ln Vitro |
Silvestrol aglycone (compound 4) inhibits MDA-MB-231 cell proliferation with an E50 of 20 ± 10 nM after 72 hours [1].
In vitro, Silvestrol aglycone inhibits myc-LUC and tub-LUC luciferase reporter protein translation with EC₅₀ values of 10 nM and 200 nM, respectively. It inhibits MDA-MB-231 breast cancer cell proliferation with an E₅₀ of 20 ± 10 nM after 72 hours. The compound induces apoptosis in LNCaP prostate cancer cells through the mitochondrial/apoptosome pathway without activating executioner caspase-3 or -7. |
| ln Vivo |
In vivo activity data for Silvestrol aglycone are limited, as the compound is primarily used as a research tool for in vitro studies. It has similar cytotoxic potency and better ADME characteristics relative to those of silvestrol, suggesting potential for in vivo applications. Further in vivo studies are needed to characterize its efficacy and safety in animal models.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Silvestrol aglycone are not typically performed, as the compound acts as a translation inhibitor rather than a traditional enzyme inhibitor. Instead, cell-free translation assays using luciferase reporter systems (myc-LUC and tub-LUC) are used to measure inhibition of protein translation. The IC₅₀ or EC₅₀ values are calculated from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for Silvestrol aglycone are performed using cancer cell lines such as MDA-MB-231, LNCaP, and others. Cells are treated with the compound at various concentrations (typically nM range) for 72 hours, and cell proliferation is assessed using MTT, CCK-8, or direct cell counting assays. Apoptosis is evaluated by measuring mitochondrial membrane potential, cytochrome c release, and caspase activity.
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| Animal Protocol |
In vivo animal experimental protocols for Silvestrol aglycone are not extensively documented. Based on its properties, the compound would likely be administered via intraperitoneal or oral routes in mouse xenograft models. Efficacy would be assessed by measuring tumor volume reduction, and toxicity would be monitored by body weight and organ histology. Further studies are needed to establish standardized protocols.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Silvestrol aglycone have not been fully characterized, but it is reported to have better ADME characteristics compared to silvestrol. The compound has a molecular weight of 478.49 and molecular formula C₂₇H₂₆O₈. It is soluble in DMSO (10 mM) and appears as a white to off-white solid powder. It should be stored at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological data for Silvestrol aglycone are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
[1]. Liu T, et al. Synthetic silvestrol analogues as potent and selective protein synthesis inhibitors. J Med Chem. 2012 Oct 25;55(20):8859-78.
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| Additional Infomation |
Silvestrol aglycone is a synthetic analogue of silvestrol with CAS number 960365-65-5, molecular formula C₂₇H₂₆O₈, and molecular weight 478.49. It inhibits protein translation initiation in cancer cells with EC₅₀ values of 10 nM (myc-LUC) and 200 nM (tub-LUC). It inhibits MDA-MB-231 cell proliferation with an E₅₀ of 20 ± 10 nM. The compound is for research use only.
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| Molecular Formula |
C27H26O8
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|---|---|
| Molecular Weight |
478.49054
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| Exact Mass |
478.163
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| CAS # |
960365-65-5
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| Related CAS # |
Silvestrol aglycone (enantiomer);1112993-18-6;Silvestrol;697235-38-4;Episilvestrol;697235-39-5
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| PubChem CID |
24178739
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| Appearance |
White to off-white solid powder
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| LogP |
2.832
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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 |
O[C@]12C3C(=CC(=CC=3O[C@@]1(C1C=CC(OC)=CC=1)[C@H](C1C=CC=CC=1)[C@H]([C@H]2O)C(=O)OC)O)OC
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| InChi Key |
HYLOONIBWUNKDH-PXIJUOARSA-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+/m1/s1
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| Chemical Name |
methyl (1R,2R,3S,3aR,8bS)-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 : ≥ 106 mg/mL (~221.53 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% 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 75.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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