EGFR/HER2/TS-IN-1

EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis[1].

Signaling Pathways >> Apoptosis >> Thymidylate Synthase

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

EGFR:0.203 μM (IC50)

HER2:0.088 μM (IC50)

Thymidylate synthase:0.168 μM (IC50)

EGFR/HER2/TS-IN-1 (Compound 4d) shows cytotoxicity with an IC50 of 0.693 μM against MCF7 cells[1]. EGFR/HER2/TS-IN-1 (10 μg, 24 h) arrests cell cycle at G2/M phase and induces cell apoptosis in MCF7 cells[1]. Cell Cycle Analysis[1] Cell Line: MCF7 Concentration: 10 μg Incubation Time: 24 h Result: Arrested cell cycle at G2/M phase. Apoptosis Analysis[1] Cell Line: MCF7 Concentration: 10 μg Incubation Time: 24 h Result: Induced cell apoptosis.

[1]. Abdellatif KRA, et al. Design, synthesis, molecular docking and antiproliferative activity of some novel benzothiazole derivatives targeting EGFR/HER2 and TS. Bioorg Chem. 2020 Aug;101:103976.