Elaiophylin
Based on 1 Customer Validation
Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
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- Purity : 97.01%
- CAS No.: 37318-06-2
- 화학식: C54H88O18
- 분자량:1025.27
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Biological Activity
제품 설명
IC50 & Target
Autophagy[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | IC50 |
31 nM
Compound: 1
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Cytotoxicity against human DU145 cells assessed as reduction in cell viability incubated for 24 hrs by FMCA method
Cytotoxicity against human DU145 cells assessed as reduction in cell viability incubated for 24 hrs by FMCA method
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[PMID: 31079965] |
| HEK293 | IC50 |
0.2 μM
Compound: 1
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Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by FMCA method
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by FMCA method
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[PMID: 31079965] |
| HeLa | IC50 |
0.19 μM
Compound: 150
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Cytotoxicity against human HeLa cells assessed as cell growth inhibition
Cytotoxicity against human HeLa cells assessed as cell growth inhibition
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[PMID: 35063731] |
| Huh-7 | IC50 |
4.2 nM
Compound: 1
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Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 24 hrs by FMCA method
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 24 hrs by FMCA method
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[PMID: 31079965] |
| MCF7 | IC50 |
0.19 μM
Compound: 150
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Cytotoxicity against human MCF7 cells assessed as cell growth inhibition
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition
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[PMID: 35063731] |
In Vitro
Elaiophylin-mediated autophagy inhibition and lysosomal dysfunction affect ovarian cancer cell survival during hypoxia. Exposure to Elaiophylin (0.025-0.5 μM; 24 hours) causes a significant increase in ovarian cancer SKOV3 cell death in hypoxia conditions[1].
In both the SKOV3 and A2780 cell lines, Elaiophylin (0.25, 0.5, 0.75 μM; 24 hours) treatment leads to significant activation of cleaved CASP9/caspase-9 and PARP1 and downregulation of BIRC5/survivin in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Ovarian cancer SKOV3 cells.
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Concentration:0.025, 0.05, 0.1, 0.2, 0.5 μM
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Incubation Time:24 hours
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Result:Caused a significant increase in ovarian cancer SKOV3 cells death in hypoxia conditions.
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Cell Line:Ovarian cancer SKOV3 cells; A2780 cells
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Concentration:0.25, 0.5, 0.75 μM
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Incubation Time:24 hours
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Result:Treatment led to significant activation of cleaved CASP9/caspase-9 and PARP1 and downregulation of BIRC5/survivin in a concentration-dependent manner.
In Vivo
Lower doses of Elaiophylin as a single agent exert significant antitumor activity, while higher doses lead to intestinal toxicity. Administration of a lower dose (2 mg/kg) of Elaiophylin as a single agent achieves a significant antitumor effect without toxicity in an orthotopic ovarian cancer model with metastasis. Toxic reactions are observed only in the 8 mg/kg group[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-wk-old BALB/C athymic mice with ovarian cancer SKOV3 cells[1]
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Dosage:1 or 2 mg/kg
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Administration:Given i.p. every 2 days for 21 days
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Result:Treatment with 2 mg/kg significantly suppressed ovarian cancer SKOV3 cells growth compared with DMSO treatment.
Chemical Information
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CAS No. 37318-06-2
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Appearance Solid
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분자량 1025.27
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화학식 C54H88O18
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Color White to off-white
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SMILES
C[C@H]1[C@@H](O)[C@@H](O)C[C@H](O[C@@H]2C[C@@]([C@H]([C@H](O)[C@H](C)[C@](OC(/C=C/C=C/[C@H](C)[C@]([C@@H](C)[C@@H](O)[C@@H]([C@]3(O)O[C@H](C)[C@@H](CC)[C@H](O[C@H]4C[C@H](O)[C@H](O)[C@H](C)O4)C3)C)([H])OC5=O)=O)([H])[C@H](/C=C/C=C/5)C)C)(O)O[C@H](C)[C@H]2CC)O1
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Synonyms
Azalomycin B; Gopalamicin; Efomycin E
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 20 mg/mL (19.51 mM; Need ultrasonic and warming; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (2.44 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
순도&문서
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Data Sheet (282 KB)
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SDS (394 KB)
- English - EN (394 KB)
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- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9754 mL | 4.8768 mL | 9.7535 mL | 24.3838 mL |
| 5 mM | 0.1951 mL | 0.9754 mL | 1.9507 mL | 4.8768 mL | |
| 10 mM | 0.0975 mL | 0.4877 mL | 0.9754 mL | 2.4384 mL | |
| 15 mM | 0.0650 mL | 0.3251 mL | 0.6502 mL | 1.6256 mL |
Elaiophylin Related Classifications
HY-15184 Related Classifications
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