EAD1
EAD1 is a Chloroquine (HY-17589A) analog with anticancer activity. EAD1 blocks autophagy, leading to the intracellular accumulation of autophagosome-related proteins LC3-II and p62. EAD1 induces cancer cell apoptosis and inhibits cancer cell proliferation. EAD1 can be used in the research of lung cancer and pancreatic cancer.
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- CAS No.: 1644388-26-0
- 화학식: C24H27Cl2N7
- 분자량:484.42
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
5.8 μM
Compound: 3h, EAD1
|
Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB method
Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB method
|
[PMID: 25699157] |
| HCC827 | IC50 |
7.6 μM
Compound: 3h, EAD1
|
Antiproliferative activity against human HCC827 cells after 72 hrs by SRB method
Antiproliferative activity against human HCC827 cells after 72 hrs by SRB method
|
[PMID: 25699157] |
| NCI-H460 | IC50 |
11 μM
Compound: 3h, EAD1
|
Antiproliferative activity against human H460 cells after 72 hrs by SRB method
Antiproliferative activity against human H460 cells after 72 hrs by SRB method
|
[PMID: 25699157] |
In Vitro
EAD1 (compound 3h) potently inhibits the proliferation of H460, HCC827 and BxPC3 cancer cells at 72 h, with IC50 values of 11 μM, 7.6 μM and 5.8 μM, respectively[1].
EAD1 (6.5-100 μM; 24 h) potently inhibits colony formation of H460 non-small cell lung cancer cells[1].
EAD1 (5-75 μM; 24 h) induces concentration-dependent apoptosis in H460 non-small cell lung cancer (NSCLC) cells[1].
EAD1 (25-50 μM; 6 h) enhances the expression of punctate LC3 in H3122 non-small cell lung cancer cells[1].
EAD1 (1-25 μM, 10 μM; 2-72 h, 24 h) induces concentration- and time-dependent accumulation of autophagy-related proteins LC3-II and p62 in H460 non-small cell lung cancer (NSCLC) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460 human NSCLC cells
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Concentration:6.5, 13, 25, 50, 100 μM
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Incubation Time:24 h
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Result:Inhibited colony formation of H460 non-small cell lung cancer cells.
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Cell Line:H460 human NSCLC cells
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Concentration:5, 25, 50, 75 μM
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Incubation Time:24 h
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Result:Induced apoptosis in H460 cells in a concentration-dependent manner.
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Cell Line:H460 human NSCLC cells
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Concentration:1, 2.5, 5, 10, 25 μM (24 h incubation); 10 μM (time-course incubation)
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Incubation Time:2, 4, 6, 24, 48, 72 h (10 μM concentration); 24 h (1-25 μM concentration)
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Result:Caused concentration- and time-dependent increases in autophagosome-bound LC3-II levels.
Showed larger increase in LC3-II levels at each tested concentration compared to HCQ.
Made the effect of 25 μM HCQ on LC3-II approximately equal to that of 5 μM EAD1.
Caused concentration-dependent accumulation of p62 (an autophagy substrate), with more potent activity than HCQ.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Autophagy
- Apoptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- MTT Cell Proliferation Assay
- Macroautophagy Solutions
Chemical Information
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CAS No. 1644388-26-0
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분자량 484.42
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화학식 C24H27Cl2N7
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SMILES
CN(CCNCC1=CN(CC2=CC=C(Cl)C=C2)N=N1)CCNC3=CC=NC4=CC(Cl)=CC=C34
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)