EGFR/HER2-IN-18 

EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC₅₀ values of 0.09 and 0.08 μM 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^[1].

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 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.

673.58

C₃₄H₂₅BrN₈OS

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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• [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]