BGC0222 is a novel prodrug of Irinotecan. BGC0222, as a PEG-cRGD-conjugated Irinotecan derivative, could slowly and steadily release Irinotecan. BGC0222 binds to α V β 3 with IC 50 values of 4.25 μM (α V β 3 ) and 58.7 μM ( α V β 5 ). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors.