| Bioactivity | EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer[1]. |
| Target | IC50: 0.122 μM (EGFR kinase), 0.078 μM (HER2 kinase), 0.585 μM (DHFR) |
| Invitro | EGFR/HER2-IN-6 (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency, and the cytotoxic potency against MCF7 cells is more potent than SOR[1].EGFR/HER2-IN-6 (0-20 μM; 0-48 h) affects cell cycle and indeces apoptosis of MCF-7 cells[1]. Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | EGFR/HER2-IN-6 (10 mg/kg; i.p. once per day for 20days) shows anti-breast cancer activity in mice[1]. Animal Model: |
| Name | EGFR/HER2-IN-6 |
| Formula | C18H21N5O3S |
| Molar Mass | 387.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sabry MA, et al. New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity. Eur J Med Chem. 2022 Aug 10;241:114661. |