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Synthesis and preliminary biological evaluation of a novel 99mTc-labeled small molecule for PD-L1 imaging.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Nov2023, Vol. 96, pN.PAG-N.PAG. 1p. - Publication Year :
- 2023
-
Abstract
- [Display omitted] In recent years, PD-1/PD-L1 checkpoint blockade immunotherapy with remarkable efficacy has set off a heat wave. The expression level of PD-L1, which plays a predictive role in anti-PD-1/PD-L1 therapy, could be quantified by noninvasive imaging with radiotracers. Herein, we introduced the synthesis and preliminary biological evaluation of a novel 99mTc-labeled small molecule radiotracer [99mTc]G 3 C-CBM for PD-L1 imaging. [99mTc]G 3 C-CBM was achieved with high radiochemical purity (>96 %) and remained good stability in PBS and FBS. In competitive combination experiment, [99mTc]G 3 C-CBM was displaced by increasing concentrations of unlabeled G 3 C-CBM, resulting in an IC 50 value of 41.25±2.23 nM for G 3 C-CBM. The uptake of [99mTc]G 3 C-CBM in A375-hPD-L1 cells (17.51±2.08 %) was approximately 6.47 folds of that in A375 cells (2.71±0.36 %) after co-incubation for 2 h. The biodistribution results showed that the radioactivity uptake in A375-hPD-L1 tumor reached the maximum (0.35±0.01 %ID/g) at 2 h post injection, and the optimum tumor/muscle ratio of 2.94±0.29 occurred at the same time. In addition, [99mTc]G 3 C-CBM was quickly cleared from the blood with a clearance half-life of just 119.25 min. These results indicate that [99mTc]G 3 C-CBM is a potential SPECT PD-L1 imaging agent and is worthy of further study. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 96
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 173630403
- Full Text :
- https://doi.org/10.1016/j.bmcl.2023.129496