Table 1

Summary of CP-751,871 characteristics

Antibody typeHuman IgG2
TargetHuman IGF-1R
Binding to human IGF-1R ECDKd = 1.5 nmol/L = 0.24 μg/mL
Inhibition of IGF1 binding to intact cellsIC50 = 1.8 nmol/L = 0.28 μg/mL
Inhibition of IGF-1R autophosphorylationIC50 = 0.42 nmol/L = 0.08 μg/mL
IGF-1R down-regulation (in vitro at 1 μg/mL)50% Reduction, 1-4 h
Specificity
Binding to insulin receptorNot detected at 3,000 μg/mL CP-751,871
Human IGF-1R (FACS)Kd = 0.6 nmol/L = 0.1 μg/mL
Cynomolgus IGF-1R (FACS)Kd = 0.5 nmol/L = 0.09 μg/ml
Rhesus monkey IGF-1R (FACS)Kd = 0.6 nmol/L = 0.1 μg/ml
Rat, dog, rabbit, marmoset IGF-1RNot detected
  • Abbreviation: FACS, fluorescence-activated cell sorting.