CYY292

CYY292 is an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, (IC₅₀s = 5.35, 4.6, 28, 28, and 78 nM, respectively).^1,2 It is selective for these kinases over FGFR4 (IC₅₀ = >1,000 nM) but also inhibits c-Kit, VEGFR2, VEGFR1, and insulin-like growth factor 1 receptor (IGF-1R; IC₅₀s = 67, 33, 36, and 75 nM, respectively), as well as EGFR, Bruton’s tyrosine kinase (BTK), cyclin-dependent kinase 4 (Cdk4)/cyclin D3, and MET (IC₅₀s = 128, 198, 214, and 396 nM, respectively).² CYY292 inhibits the proliferation of MG-63, U2OS, MNNG/HOS, and Saos-2 osteosarcoma cells (IC₅₀s = 0.84, 0.76, 1.36, and 0.72 µM, respectively).¹ It inhibits the migration and invasion of U87MG and LN-229 glioblastoma cells when used at concentrations of 0.3 and 0.5 µM.² CYY292 (30 mg/kg) decreases tumor volume and increases survival in a U87MG orthotopic mouse xenograft model.

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1. Chen, X., Liu, L., Liu, P., et al. Discovery of potent and orally bioavailable platelet-derived growth factor receptor (PDGFR) inhibitors for the treatment of osteosarcoma. J. Med. Chem. 65(7), 5374-5391 (2022).

2. Bi, Y., Zheng, R., Hu, J., et al. A novel FGFR1 inhibitor CYY292 suppresses tumor progression, invasion, and metastasis of glioblastoma by inhibiting the Akt/GSK3b/ snail signaling axis. Genes Dis. 11(1), 479-494 (2023).