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-Bombesin heterodimer designed as a radiotheranostic probe for prostate cancer

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1

Synthesis and preclinical evaluation of the

177

Lu-DOTA-PSMA(inhibitor)-Lys

3

-Bombesin heterodimer designed as a radiotheranostic probe for prostate cancer

Alondra Escudero-Castellanos1,2, Blanca Ocampo-García1*, Guillermina Ferro-Flores1, Clara Santos-Cuevas1, Enrique Morales-Ávila3, Myrna Luna-Gutiérrez1, Keila Isaac-Olivé2.

1Departamento de Materiales Radiactivos. Instituto Nacional de Investigaciones Nucleares, Ocoyoacac, 52750, Estado de México, MEXICO.

2Facultad de Medicina. Universidad Autónoma del Estado de México, Toluca, Estado de México 50180, MEXICO.

3Facultad de Química. Universidad Autónoma del Estado de México, Toluca, Estado de México 50180, MEXICO.

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2 Figure 1: DOTA-iPSMA-BN structure

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3 Figure 2. FT-IR spectrum of iPSMA-BN.

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4 Figure 3. Chemical characterization by mass spectroscopy (MALDI as ionization

technique) of synthesized iPSMA-BN.

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5 Figure 4. Chemical characterization by 1H–NMR spectrum of synthesized iPSMA-BN.

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6 Figure 5. Chemical characterization byreverse phase HPLC analysis of synthesized

iPSMA-BN (=265 nm).

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7 Figure 6. Stability against serum proteins of 177Lu-iPSMA-BN. a) HPLC chromatogram of human serum at 280 nm b) HPLC radio-chromatogram at 0.5, 3 and 24 h of incubation of in serum. The radiopharmaceutical demonstrated stability in human serum and protein binding of 1.88 %, 1.93 %, 2.47 % at 0.5, 3 and 24 h, respectively.

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