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FIIN-2
- Development stage
- Preclinical
- Lead developer
- Dana-Farber Cancer Institute
- Modality
- Small Molecules
01
Overview
FIIN-2 is an irreversible, pan-fibroblast growth factor receptor (FGFR) inhibitor developed as a next-generation small molecule to overcome resistance to first-generation clinical FGFR inhibitors such as BGJ398 and AZD4547. It functions as a covalent inhibitor, forming a stable bond with Cys491 of FGFR2 and exhibiting a DFG-out binding mode. FIIN-2 is notable for its ability to potently inhibit the proliferation of cells dependent on gatekeeper mutants of FGFR1 or FGFR2, which typically confer resistance to earlier non-covalent inhibitors. While currently a research compound, it has shown potential for treating FGFR-dependent malignancies, including breast cancer, hepatocellular carcinoma, and prostate cancer.
- Other names
- CAS 1633044-56-0CAS1633044-56-0CAS-1633044-56-0
02
Targets
FGFR4 (Fibroblast growth factor receptor 4)FGFR3 (Fibroblast growth factor receptor 3)EGFR T790M (Epidermal growth factor receptor T790M mutant)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)
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