EGFR/HER2-IN-20
EGFR/HER2-IN-20 is a dual EGFR/HER2 inhibitor. EGFR/HER2-IN-20 induces G1/S phase cell cycle arrest by downregulating CCND1. EGFR/HER2-IN-20 induces cell apoptosis by upregulating BAX and caspase-3. EGFR/HER2-IN-20 inhibits cancer cell migration. EGFR/HER2-IN-20 can be used in the research of cervical cancer and breast cancer.
For research use only. We do not sell to patients.
- Formula: C22H15FN4O2
- Molecular Weight:386.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Bax |
Caspase 3 |
EGFR/HER2-IN-20 (Compound 2b) potently inhibits the proliferation of HeLa and MDA-MB-231 cancer cells, with IC50 values of 3.87 μM and 3.01 μM, respectively; meanwhile, this compound exhibits high selectivity toward WI-38 normal cells, with selectivity indices of 22.27 and 28.63, respectively[1].
EGFR/HER2-IN-20 induces G1/S phase cell cycle arrest and significant apoptosis in HeLa cells, increasing the proportion of total apoptotic cells to 28.42%. It also alters cell cycle distribution, leading to cell accumulation in the G0/G1 and S phases, while reducing the number of cells in the G2/M phase[1].
EGFR/HER2-IN-20 (72 h) significantly inhibits the migration of MDA-MB-231 cells and reduces the wound healing rate to 62.96%[1].
EGFR/HER2-IN-20 upregulates the expression levels of pro-apoptotic proteins BAX and caspase-3 by 7.42-fold and 9.16-fold, respectively, and downregulates the expression level of CCND1 protein to 0.23-fold in HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 386.38
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Formula C22H15FN4O2
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SMILES
O=C1NC(C2=CC=C(F)C(C#N)=C2)N(C(CC3=CC=CC=N3)=O)C4=CC=CC=C41
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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
[1]. El-Hema HS, et al.. Rationally designed quinazolinone derivatives incorporating acetyl pyridine and thiazole scaffolds as dual EGFR/HER-2 anticancer agents: integrated biological evaluation, molecular profiling, and advanced computational studies. Bioorganic chemistry. 2026 Sep 05;179:110052. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)