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FIIN-4 is a first-in-class, orally active, covalent pan-FGFR inhibitor that targets a conserved cysteine in the P-loop of FGFR1-4. It exhibits potent inhibitory activity against FGFR1, FGFR2, FGFR3, and FGFR4 with IC50 values of 2.6 nM, 2.6 nM, 5.6 nM, and 9.2 nM, respectively. Developed by researchers at Dana-Farber Cancer Institute and Purdue University, FIIN-4 has demonstrated preclinical efficacy in overcoming drug resistance (such as resistance to trastuzumab emtansine or lapatinib) and inhibiting metastatic tumor growth in breast cancer models, particularly within the pulmonary microenvironment.
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