EGFR-IN-174
EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer.
For research use only. We do not sell to patients.
- Formula: C16H23N3O2S3
- Molecular Weight:385.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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VEGFR-2 0.2007 μM (IC50) |
EGFR-IN-174 (compound 3a) (2 days) displays strong cytotoxicity against HCT-116, HepG-2, and MCF-7 Cell Lines (IC50 = 5.58, 4.82 and 11.15 μM, respectively) coupled with minimal cytotoxicity against normal WI-38 cells (IC50 = 86.26 μM)[1].
EGFR-IN-174 (4.82-11.15 μM, 72 h) effectively induces cell cycle arrest at both the G2/M and Pre-G1 phases, and significantly triggers apoptosis in HCT-116, HepG-2, and MCF-7 Cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, HepG-2, and MCF-7 Cells
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Concentration:5.58, 4.82, and 11.15 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
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Incubation Time:72 h
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Result:Induced a significant increase in the Hep-G2 cell population in the G2/M (from 12.73% to 34.85%) and Pre-G1 (from 1.92% to 11.82%) phases.
Induced a significant increase in the HCT-116 cell population in the G2/M (from 5.45% to 29.21%) and Pre-G1 (from 1.91% to 11.22%) phases.
Significantly increased the population of MCF-7 Cells in the G2/M and Pre-G1 phases from 9.55% and 2.14% to 35.31% and 15.52%, respectively.
Reduced the proportion of cells in the G0-G1 and S phases compared to the control in Hep-G2, HCT-116, and MCF-7 cell lines.
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Cell Line:HCT-116, HepG-2, and MCF-7 Cells
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Concentration:5.58, 4.82, and 11.15 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
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Incubation Time:72 h
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Result:Induced a total apoptosis rate of 11.22 % in HCT-116 cells (early: 3.62%; late: 6.24%).
Induced a total apoptosis rate of 11.82 % in HepG-2 cells (early: 3.59%; late: 6.65%).
Induced a total apoptosis rate of 15.52 % in MCF-7 cells (early: 4.49%; late: 8.88%).
Chemical Information
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Molecular Weight 385.57
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Formula C16H23N3O2S3
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SMILES
S=C(N/N=C(C1=CC=C(S(=O)(N2CCC(C)CC2)=O)C=C1)\C)SC
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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)