The chlorambucil l-histidine conjugate was synthesized and radiolabeled with [99mTc (CO) 3]+ core to form the 99mTc (CO) 3 (His–CB) complex. The radiochemical purity of the complex was over 90%. It had good hydrophilicity and was stable at room temperature. The high initial tumor uptake with certain retention, fast clearance from background, good tumor/non-tumor ratios and satisfactory scintigraphic images highlighted the potential of ...