TABLE 1

Kinase-selectivity profile of SOMG-833

IC50 values are shown as the mean ± S.D. or estimated values from three separate experiments.

Tyrosine KinaseIC50Tyrosine KinaseIC50
nMnM
c-MET0.93 ± 0.15RET>10,000
RON>10,000EGFR>10,000
Axl>10,000ErbB2>10,000
Tyro-3>10,000ErbB4>10,000
ALK>10,000c-Src>10,000
Flt-1>10,000ABL>10,000
KDR>10,000EPH-A2>10,000
c-Kit>10,000EPH-B2>10,000
PDGFRα>10,000IGF1R>10,000
PDGFRβ>10,000FGFR1>10,000
  • ABL, Abelson murine leukemia viral oncogene homolog 1; Axl, tyrosine-protein kinase receptor UFO; c-Kit, tyrosine-protein kinase kit; c-Src, tyrosine-protein kinase CSK; EGFR, epidermal growth factor receptor; EPH, Ephrin-type receptor; ErbB2 (HER2), human epidermal growth factor receptor 2; ErbB3, human epidermal growth factor receptor 3; FGFR1, fibroblast growth factor receptor 1; Flt-1, vascular endothelial growth factor receptor 1; IGF1R1, insulin-like growth factor 1; VEGFR2, vascular endothelial growth factor receptor 2; PDGFR, platelet-derived growth factor receptor; RET, rearranged during transfection tyrosine kinase; RON, macrophage-stimulating protein receptor; Tyro-3, tyrosine-protein kinase receptor.