EGFR/HER2-IN-21
EGFR/HER2-IN-21 is an EGFR/HER2 tyrosine kinase inhibitor (IC50 = 0.058 and 0.060 µM, respectively). EGFR/HER2-IN-21 inhibits VEGFR-2 kinase activity with an IC50 of 0.51 µM. EGFR/HER2-IN-21 induces apoptosis and activates caspase 3 and caspase 7. EGFR/HER2-IN-21 exhibits antiproliferative activity against cancer cells. EGFR/HER2-IN-21 can be used for research on breast adenocarcinoma, hepatocellular carcinoma, and colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C21H18N4O2S
- Molecular Weight:390.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
EGFR 0.058 μM (IC50) |
HER2 0.06 μM (IC50) |
VEGFR2 0.51 μM (IC50) |
Caspase 3 |
Caspase-7 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
5.20 μM
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Antiproliferative activity against human HCT-116 colorectal carcinoma cells assessed as viability reduction by MTT colorimetric assay.
Antiproliferative activity against human HCT-116 colorectal carcinoma cells assessed as viability reduction by MTT colorimetric assay.
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42706361 |
| MCF7 | IC50 |
4.20 μM
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Antiproliferative activity against human MCF-7 breast adenocarcinoma cells assessed as viability reduction by MTT colorimetric assay.
Antiproliferative activity against human MCF-7 breast adenocarcinoma cells assessed as viability reduction by MTT colorimetric assay.
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42706361 |
| HepG2 | IC50 |
3.20 μM
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Antiproliferative activity against human HepG-2 hepatocellular carcinoma cells assessed as viability reduction by MTT colorimetric assay.
Antiproliferative activity against human HepG-2 hepatocellular carcinoma cells assessed as viability reduction by MTT colorimetric assay.
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42706361 |
| WI-38 | IC50 |
51.21 μM
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Cytotoxicity against normal human diploid WI-38 cells assessed by MTT assay.
Cytotoxicity against normal human diploid WI-38 cells assessed by MTT assay.
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42706361 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG-2
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Concentration:3.20 µM
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Incubation Time:24 h
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Result:Exposure to EGFR/HER2-IN-21 (compound 6b) at its IC50 concentration resulted in a 6.9-fold increase in luminescence compared with control cells.
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Liver Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Molecular Weight 390.46
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Formula C21H18N4O2S
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SMILES
OC(C1=CC(C)=CC=C1N2)=C(/C=N/N=C3SC=C(C)N\3C4=CC=CC=C4)C2=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR/HER2-IN-21 Related Classifications
HY-189725 Related Classifications
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