NOTA is a multifunctional chelator capable of forming stable complexes with metal ions and is commonly used in radiopharmaceuticals, molecular imaging and targeted nuclear therapy.

CXCR4 (Jurkat T cells):14.9  nM, αvβ₃ integrin:27.9  nM

[⁶⁴Cu]NOTA-pentixather showed high affinity for CXCR4 in Jurkat T cells (IC₅₀ = 14.9 ± 2.1 nM) and was efficiently internalized in Chem-1 cells stably expressing human CXCR4[1].[⁶⁸Ga]NOTA-RGD showed a high binding affinity for the αvβ₃ integrin (IC₅₀ = 27.9 ± 6.8 nM) in receptor binding assays, indicating effective targeting of integrin expression associated with angiogenesis[2].

In SCID mice bearing Daudi lymphoma, intravenous injection of [⁶⁴Cu]NOTA-pentixather resulted in high tumor uptake (13.1 ± 1.5% ID/g at 1.5 h post-injection), exceeding uptake in all other organs[1].