CYB-5067

CYB-5067 (1.5-10000 nM, 0.123-3.3 μM; 24 h) potently and rapidly degrades FGFR2 in KATO III cells with a DC₅₀ of 27 nM and 96% maximum degradation, achieving sustained target suppression following washout^[1].
CYB-5067 (0.0001-10 μM; 72 h) inhibits KATO III cell proliferation with an IC₅₀ of 3.8 nM, showing greater potency than Infigratinib (HY-13311)^[1].
CYB-5067 can covalently recruit RNF213 in KATO III and HEK293T cells, forming a ternary complex with FGFR2. This mediates RNF213-dependent FGFR2 ubiquitination and proteasome degradation, independent of NEDD8-mediated E3 ligase activation and lysosomal pathways^[1].
CYB-5067 covalently engages RNF213 at the solvent-exposed C1748 residue, which is required for productive recruitment of RNF213^[1].
CYB-5067 (0.123-10 μM; 16 h, 0.0001-10 μM; 72 h) acts as a pan-FGFR degrader, potently degrading FGFR1-4 in subtype-specific and multi-subtype cell models with subtype-dependent potency^[1].
CYB-5067 (0.5 μM; 12 h) specifically downregulates FGFR2 in KATO III cells at the proteome level, with other observed protein changes being target-driven downstream effects^[1].
CYB-5067 (0.123-10 μM; 16 h, 0.0001-10 μM; 72 h) potently degrades FGFR2 and inhibits proliferation in SNU-16 and Ba/F3-ETV6-FGFR2 cells, with high potency in the FGFR2 fusion-positive Ba/F3 model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.