Gefitinib-based PROTAC 3是一种创新型的PROTAC，通过将Gefitinib与E3泛素连接酶相结合，专门靶向并降解受体酪氨酸激酶（RTK）。Gefitinib-based PROTAC 3在治疗包括耐药性癌症在内的多种癌症中展现了显著的研究潜力。

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib. MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. It is bioavailable in mice following ip administration.