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111in incl3

Manufactured by Mallinckrodt
Sourced in Switzerland

[111In]InCl3 is a radioactive compound containing the radioisotope indium-111 (111In). It is a gamma-emitting radionuclide with a half-life of approximately 2.8 days. This product is intended for use as a raw material in the production of radiopharmaceuticals.

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4 protocols using 111in incl3

1

Radiolabeling of FnBPA5 and Scrambled FnBPA5

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FnBPA5 and FnBPA5 scr equipped with a NODAGA-chelator were radiolabeled with [111In]InCl3 (Mallinckrodt, Cham, Switzerland) in metal-free ammonium acetate (0.5 M, pH 5.5) at a molar activity of 6 MBq/nmol. After 30 min incubation at 50 °C, the solution was subjected to quality control using RP-HPLC (Agilent 1200 Series, Santa Clara, USA) connected to a GinaStar Elysia-Raytest γ-detector (Straubenhardt, Germany). A C18 column (ReproSil-Pur 120, 3 μm, Dr. Maisch GmbH, Germany) was used and eluted with a linear gradient ranging from 95 to 5% of solvent A in 10 min (A: H2O containing 0.1% trifluoroacetic acid (TFA); B: acetonitrile). Typically, radiolabeling efficiencies of > 95% were achieved. Typical HPLC chromatograms of [111In]In-FnBPA5 and [111In]In-FnBPA5 scr are shown in Additional file 1: Figure S1.
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2

Production and Characterization of Radionuclides

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Solutions of [18F]F, [64Cu]CuCl2 and [131Ba]Ba(NO3)2 were produced in‐house by proton bombardment of the respective liquid or solid target at the TR‐FLEX Cyclotron from ASCI.30 All cyclotron‐based radionuclides are non‐carrier‐added products. [224Ra]Ra(NO3)2 was separated from a 228Th‐source by ion exchange chromatography and was obtained as non‐carrier‐added solution. [177Lu]LuCl3 was purchased by ITG and [111In]InCl3 by Mallinckrodt. [89Zr]Zr(C2O4)2 was purchased by Perkin Elmer and [133Ba]BaCl2 from Polatom. The specific activity from the manufacturers’ certificate was 50 MBq/mg Ba. Activity count rates were measured using the ISOMED 2160 (MED) sodium iodide detector and the ISOMED 2100 dose calibrator (MED). High‐precision measurements were performed using a HPGe detector by Canberra.
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3

Synthesis and Radiolabeling of PSMA I&T

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The synthesis of PSMA I&T (DOTAGA-(I-y)fk(Sub-KuE) was performed as described previously. 13 For 111 In-labeling, 500 μL of [ 111 In]InCl 3 (SA >205 GBq/μmol; Mallinckrodt Pharmaceuticals, Dublin, Ireland) was added to 14 μL PSMA I&T (1.0 mM in water) in 600 μL sodium acetate buffer (0.15 M, pH 5.7). After heating to 95°C for 25 minutes, labeling was quantitative. The reaction mixture was purified over a Waters Sep Pak C18 light cartridge (Waters Corporation, Milford, MA). The final product was dissolved in 8.5 mL phosphate-buffered saline with subsequent sterile filtration.
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4

Radiolabeling of Ex4 and Derivatives

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Ex4 and its cleavable linker derivatives were radiolabelled with [111In]InCl3 (Mallinckrodt, Cham, Switzerland) in the presence of 0.5 M ammonium acetate pH 5.5 at a specific activity of 4 MBq/nmol. To prevent oxidation of Met in the radiolabelling solution, D-L-Selenomethionine was added in a 50-fold molar excess to all solutions carrying a Met in their sequence. The radiolabelling mixtures were incubated for 15 min at 50 °C and subjected to reverse phase high pressure liquid chromatography (RP-HPLC, Agilent 1200 Series, Santa Clara, USA) connected to a GinaStar raytest γ-detector (Elysia Raytest, Straubenhardt, Germany). A C18 column (ReproSil-Pur 120, 3 μm, Dr. Maisch GmbH, Germany) with a linear gradient ranging from 95 to 5% of solvent A in 10 min (A: H2O containing 0.1% trifluoracetic acid (TFA); B: acetonitrile (MeCN)) was employed.
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