《225Ac-H4py4pa for Targeted Alpha Therapy》 was written by Li, Lily; Rousseau, Julie; Jaraquemada-Pelaez, Maria de Guadalupe; Wang, Xiaozhu; Robertson, Andrew; Radchenko, Valery; Schaffer, Paul; Lin, Kuo-Shyan; Benard, Francois; Orvig, Chris. Product Details of 1195-59-1 And the article was included in Bioconjugate Chemistry in 2021. The article conveys some information:
Herein, we present the syntheses and characterization of a new undecadendate chelator, H4py4pa, and its bifunctional analog H4py4pa-phenyl-NCS, conjugated to the monoclonal antibody, Trastuzumab, which targets the HER2+ cancer. H4py4pa possesses excellent affinity for 225Ac (α, t1/2 = 9.92 d) for targeted alpha therapy (TAT), where quant. radiolabeling yield was achieved at ambient temperature, pH = 7, in 30 min at 10-6 M chelator concentration, leading to a complex highly stable in mouse serum for at least 9 d. To investigate the chelation of H4py4pa with large metal ions, lanthanum (La3+), which is the largest nonradioactive metal of the lanthanide series, was adopted as a surrogate for 225Ac to enable a series of nonradioactive chem. studies. In line with the 1H NMR spectrum, the DFT (d. functional theory)-calculated structure of the [La(py4pa)]- anion possessed a high degree of symmetry, and the La3+ ion was secured by two distinct pairs of picolinate arms. Furthermore, the [La(py4pa)]- complex also demonstrated a superb thermodn. stability (log K[La(py4pa)]- ~20.33, pLa = 21.0) compared to those of DOTA (log K[La(DOTA)]- ~24.25, pLa = 19.2) or H2macropa (log K[La(macropa)]- = 14.99, pLa ~8.5). Moreover, the functional versatility offered by the bifunctional py4pa precursor permits facile incorporation of various linkers for bioconjugation through direct nucleophilic substitution. In this work, a short phenyl-NCS linker was incorporated to tether H4py4pa to Trastuzumab. Radiolabeling studies, in vitro serum stability, and animal studies were performed in parallel with the DOTA-benzyl-Trastuzumab. Both displayed excellent in vivo stability and tumor specificity. The results came from multiple reactions, including the reaction of 2,6-Pyridinedimethanol(cas: 1195-59-1Product Details of 1195-59-1)
2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. Pyridine and its simple derivatives are stable and relatively unreactive liquids, with strong penetrating odours that are unpleasant.Product Details of 1195-59-1
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