BMS-754807 is an orally bioavailable, potent and reversible small molecule inhibitor of the IGF-1R/IR family kinases with Ki <2 nmol/L. BMS-754807 could effectively inhibit the growth of many human tumor types from in vitro perspective, such as mesenchymal, hematopoietic and epithelial tumor cell lines with an IC50 value of 5–365 nmol/L. BMS-754807 F-18 is the first small molecule radioligand that showed promise for imaging IGF-1R in tumor/ cancer. The results indicate that BMS-754807 F-18 can be a potential PET imaging agent for in vivo monitoring IGF-1R.