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PD173074
- Development stage
- Preclinical
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral (preclinical, Animal), In Vitro (lab/research Use Only)
01
Overview
PD173074 is a potent, selective, ATP-competitive *small molecule inhibitor* of the fibroblast growth factor receptor (FGFR) tyrosine kinase family, with strong activity against FGFR1 and FGFR3, and effective inhibition of FGFR2, FGFR4, and VEGFR2[1][5][7][8][9]. PD173074 inhibits FGFR autophosphorylation and downstream signaling, blocking FGF-driven cellular proliferation, differentiation, and angiogenesis without significant cytotoxicity outside FGFR pathways[1][3][8]. It can reverse ABCB1-mediated multidrug resistance by modulating transporter activity[3]. Preclinical studies show PD173074 can suppress tumor growth and angiogenesis in multiple models, including small cell lung cancer and myeloma, with increased apoptosis in tumor cells and extension of survival, but it has not entered clinical trials and its development has been discontinued at the preclinical stage[1].
- Brand names
- PD173074PD-173074PD 173074
- Other names
- PD173074PD-173074PD 173074UNII-A4TLL8634YUNII-A-4TLL8634YUNII-A 4TLL8634Y
02
Targets
FGFR4 (Fibroblast growth factor receptor 4)VEGFR2 (Vascular endothelial growth factor receptor 2)ABCB1 (P-glycoprotein)FGFR3 (Fibroblast growth factor receptor 3)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)
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