EGFR/HER2-IN-18
EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 (EGFR) and 0.08 μM (HER2) respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer.
For research use only. We do not sell to patients.
- Formula: C34H25BrN8OS
- Molecular Weight:673.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All EGFR Isoforms
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Biological Activity
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HER2 0.08 μM (IC50) |
EGFR/HER2-IN-18 (Compound 10f) (24 h) exhibits good cytotoxic IC50 levels against different cancer cell lines such as HePG-2 (3.90 μM), HCT-116 (7.35 μM) and MCF-7 (2.84 μM)[1].
EGFR/HER2-IN-18 achieves highly potent cytotoxic IC50 levels against all the resistant cell lines as follows: 6.971 μM for SKBr3 (Lapatinib (HY-50898) IC50 = 9.614 μM), 2.769μM for BT474 (Lapatinib IC50 = 23.691 μM), and 11.472 μM for MDA-MB-453 (Lapatinib IC50 = 29.762 μM)[1].
EGFR/HER2-IN-18 (39.8 μg/mL, 48 h) induces apoptosis of MCF-7 cells[1].
EGFR/HER2-IN-18 (48 h) exhibits G0/G1 phase cell cycle ar¬ rest with 77 % cells compared with 70 % in control in 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:MCF-7
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Concentration:39.8 μg/ml
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Incubation Time:48 h
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Result:Resulted in a significant increase in the percentage of both early (Q4) and late apoptosis (Q2) from 11 to 25%, respectively.
Counteracted apoptosis to a similar extent as the positive control (Lapatinib).
Chemical Information
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Molecular Weight 673.58
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Formula C34H25BrN8OS
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SMILES
O=C(N/N=C1SC=C(C2=CC=C(C)C=C2)N/1C3=CC=C(Br)C=C3)C4=CC=CC(NC5=C6C(N(C7=CC=CC=C7)N=C6)=NC=N5)=C4
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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]. Salem IM, et al. Exploitation of novel pyrazolo[3,4-d]pyrimidine scaffold tethered to thiazole as potential EGFR/HER2 dual kinase inhibitor to overcome lapatinib resistant breast cancer: Design, synthesis, in silico docking and molecular dynamic simulation. Bioorg Chem. 2025 Jun 3;163:108671. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR/HER2-IN-18 Related Classifications
HY-174414 Related Classifications
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