Episilvestrol
Based on 1 publication(s) in Google Scholar
Episilvestrol is a derivative of silvestrol, isolated from the fruits and twigs of Aglaia perviridis, and is a specific eIF4A-targeting translation inhibitor, with antitumor activity.
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- Purity: 99.86%
- CAS No.: 697235-39-5
- 화학식: C34H38O13
- 분자량:654.66
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Episilvestrol
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Biological Activity
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eIF4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>20 μM
Compound: 7
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Inhibition of NF-kappaB p65 isolated from nuclear extract of human HeLa cells assessed as blockade of binding to biotinylated consesus sequence by chemiluminescence assay
Inhibition of NF-kappaB p65 isolated from nuclear extract of human HeLa cells assessed as blockade of binding to biotinylated consesus sequence by chemiluminescence assay
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[PMID: 20939540] |
| HeLa | IC50 |
0.02 μM
Compound: 8
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Antiproliferative activity against human HeLa cells assessed as cell growth inhibition by [35S] methionine incorporation assay
Antiproliferative activity against human HeLa cells assessed as cell growth inhibition by [35S] methionine incorporation assay
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[PMID: 33592144] |
| HL-60 | IC50 |
4 nM
Compound: 8
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Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
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[PMID: 33592144] |
| HT-29 | IC50 |
0.004 μM
Compound: Silvestrol
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Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay
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[PMID: 21513293] |
| Kasumi 1 | IC50 |
24 nM
Compound: Silvestrol
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Cytotoxicity against human Kasumi-1 cells incubated for 48 hrs by MTS assay
Cytotoxicity against human Kasumi-1 cells incubated for 48 hrs by MTS assay
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[PMID: 27983842] |
| LNCaP | ED50 |
1.5 nM
Compound: 13
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Growth inhibition of human LNCAP cells xenografted in ip dosed NCr nu/nu mouse administered once daily from day 3 to 6 after implantation measured on day 7 by MTT-based hollow-fiber test
Growth inhibition of human LNCAP cells xenografted in ip dosed NCr nu/nu mouse administered once daily from day 3 to 6 after implantation measured on day 7 by MTT-based hollow-fiber test
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[PMID: 19161316] |
| Lu1 | ED50 |
1.2 nM
Compound: 13
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Growth inhibition of human Lu1 cells xenografted in ip dosed NCr nu/nu mouse administered once daily from day 3 to 6 after implantation measured on day 7 by MTT-based hollow-fiber test
Growth inhibition of human Lu1 cells xenografted in ip dosed NCr nu/nu mouse administered once daily from day 3 to 6 after implantation measured on day 7 by MTT-based hollow-fiber test
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[PMID: 19161316] |
| MCF7 | ED50 |
1.5 nM
Compound: 13
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Growth inhibition of human MCF7 cells xenografted in ip dosed NCr nu/nu mouse administered once daily from day 3 to 6 after implantation measured on day 7 by MTT-based hollow-fiber test
Growth inhibition of human MCF7 cells xenografted in ip dosed NCr nu/nu mouse administered once daily from day 3 to 6 after implantation measured on day 7 by MTT-based hollow-fiber test
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[PMID: 19161316] |
| MDA-MB-231 | EC50 |
0.8 nM
Compound: 1
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Inhibition of eIF4FA in human MDA-MB-231 cells transfected with c-myc- 5'-UTR-luciferase construct assessed as reduction in translation initiation incubated for 24 hrs by differential translation assay
Inhibition of eIF4FA in human MDA-MB-231 cells transfected with c-myc- 5'-UTR-luciferase construct assessed as reduction in translation initiation incubated for 24 hrs by differential translation assay
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[PMID: 23025805] |
| MDA-MB-231 | EC50 |
3 nM
Compound: 1
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Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTS assay
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTS assay
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[PMID: 23025805] |
| MDA-MB-231 | EC50 |
7 nM
Compound: 1
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Inhibition of eIF4FA in human MDA-MB-231 cells transfected with tubulin 5'-UTR-luciferase construct assessed as reduction in translation initiation incubated for 24 hrs by differential translation assay
Inhibition of eIF4FA in human MDA-MB-231 cells transfected with tubulin 5'-UTR-luciferase construct assessed as reduction in translation initiation incubated for 24 hrs by differential translation assay
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[PMID: 23025805] |
| MDA-MB-435 | IC50 |
0.006 μM
Compound: Silvestrol
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Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTS assay
Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTS assay
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[PMID: 21513293] |
| MV4-11 | IC50 |
11 nM
Compound: Silvestrol
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Cytotoxicity against human MV4-11 cells incubated for 48 hrs by MTS assay
Cytotoxicity against human MV4-11 cells incubated for 48 hrs by MTS assay
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[PMID: 27983842] |
| NB-4 | IC50 |
4 nM
Compound: 8
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Antiproliferative activity against human NB-4 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
Antiproliferative activity against human NB-4 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
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[PMID: 33592144] |
| OCI-AML2 | IC50 |
4 nM
Compound: 8
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Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
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[PMID: 33592144] |
| OCI-AML-3 | IC50 |
4 nM
Compound: 8
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Antiproliferative activity against human OCI-AML-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
Antiproliferative activity against human OCI-AML-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
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[PMID: 33592144] |
| U-937 | IC50 |
4 nM
Compound: 8
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Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 48 hrs by MTS assay
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[PMID: 33592144] |
Episilvestrol is a specific eIF4A-targeting translation inhibitor, with antitumor activity[1]. Episilvestrol is cytotoxic activity against several human cancer cell lines, such as Lu1, LNCaP, MCF-7 and HUVEC cells, with ED50s of 3.8, 3.8, 5.5 and 15.3 nM, respectively[2]. The GI50s of Episilvestrol against the cell proliferation of NCI-H460 and MCF-7 cels are 17.96 nM and 17.96 nM after first test and 15.6 nM and 18.7 nM after 2 months via SRB assay. Episilvestrol also suppresses HK1 cells and EBV-positive C666.1 NPC cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 697235-39-5
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Appearance Solid
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분자량 654.66
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화학식 C34H38O13
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Color White to off-white
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SMILES
O=C([C@H]([C@H]1C2=CC=CC=C2)[C@@H](O)[C@]3(O)[C@@]1(C4=CC=C(OC)C=C4)OC5=CC(O[C@@H]6O[C@@H]([C@@H](O)CO)CO[C@H]6OC)=CC(OC)=C35)OC
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 25 mg/mL (38.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
A total of 1×104 HK1 cells/well or 3×104 C666.1 cells/well are seeded into 96-multiwell microtiter plates. At 24 h following seeding, the medium is aspirated and replaced with fresh medium containing various concentrations of silvestrol or Episilvestrol. Vehicle control cultures receive DMSO alone. The cells are then incubated for 24 h at 37°C in an atmosphere containing 5% CO2. The number of viable cells at the end of the incubation period is measured using MTS assay. Absorbance at 490 nm is read and subtracted with non-specific absorbance measured at 630 nm. Wells containing medium without cells serve as blanks. Cell viability is calculated as a percentage compared to the control cells, which are arbitrarily assigned 100% viability. The half maximal inhibitory concentration (IC50) values are graphically obtained from the dose-response curves[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Chambers JM, et al. Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II. Org Lett. 2013 Mar 15;15(6):1406-9. [Content Brief]
[2]. Hwang BY, et al. Silvestrol and episilvestrol, potential anticancer rocaglate derivatives from Aglaia silvestris. J Org Chem. 2004 May 14;69(10):3350-8. [Content Brief]
[3]. Daker M, et al. Inhibition of nasopharyngeal carcinoma cell proliferation and synergism of cisplatin with silvestrol and episilvestrol isolated from Aglaia stellatopilosa. Exp Ther Med. 2016 Jun;11(6):2117-2126. Epub 2016 Mar 29. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5275 mL | 7.6376 mL | 15.2751 mL | 38.1878 mL |
| 5 mM | 0.3055 mL | 1.5275 mL | 3.0550 mL | 7.6376 mL | |
| 10 mM | 0.1528 mL | 0.7638 mL | 1.5275 mL | 3.8188 mL | |
| 15 mM | 0.1018 mL | 0.5092 mL | 1.0183 mL | 2.5459 mL | |
| 20 mM | 0.0764 mL | 0.3819 mL | 0.7638 mL | 1.9094 mL | |
| 25 mM | 0.0611 mL | 0.3055 mL | 0.6110 mL | 1.5275 mL | |
| 30 mM | 0.0509 mL | 0.2546 mL | 0.5092 mL | 1.2729 mL |
Episilvestrol Related Classifications
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