Abstract: Provided herein are [18F]-labeled compounds having a chemical structure: R1 is 18F, 1-piperazinyl-4-CH2CH2—18F or 1-piperazinyl-4-CH2CH2OCH2CH2—18F, R2 is CH3 or 18F and R3 is Cl or 18F, such that only one of R1, R2 and R3 comprise an 18F. Also provided are methods for in vivo imaging using the [18F]-labeled compounds, particularly methods of imaging utilizing positron emission tomography. These methods are effective for diagnosing a pathophysiological condition susceptible to treatment with kinase inhibitor(s) in a subject, or for determining whether a cancer in a subject that is susceptible to being treated with a kinase inhibitor has developed resistance or increased sensitivity to the same and for maximizing tumor response to akinase inhibitor with minimal toxicity to the subject.

Abstract: There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the —PR2 containing biomolecules by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a —PR2 containing biomolecule.