Journal: bioRxiv

Article Title: [ 123 I]Italia: A PARP-Directed Auger Electron-Emitting Agent for Targeted Radionuclide Therapy of Cancer

doi: 10.64898/2026.03.13.711622

Figure Lengend Snippet: A) Uptake of [ 123 I]Italia_A in PSN-1 cells at different time points. B) Efflux of [ 123 I]Italia_A in PSN1 cells. C) Comparison of u ptake and blocking of [ 123 I]Italia_A, B and racemic mix. in PSN-1, cas1, KO cells after 1 hour exposure. D) Comparison of b locking of [ 123 I]Italia_A, B and racemic mix. uptake in PSN-1 cells by panel of PARP inhibitors.

Article Snippet: Human pancreatic adenocarcinoma cells (PSN-1), and human prostate cancer cells (PC-3) were purchased from ATCC; the murine breast cancer cell line 4T1 was a kind gift from prof. Nicola Sibson, Department of Oncology, University of Oxford.

Techniques: Comparison, Blocking Assay

Journal: bioRxiv

Article Title: [ 123 I]Italia: A PARP-Directed Auger Electron-Emitting Agent for Targeted Radionuclide Therapy of Cancer

doi: 10.64898/2026.03.13.711622

Figure Lengend Snippet: A) IC 50 in PSN-1 cells (IC 50 : 2.85 nM, 95%CI: 1.98 nM-4.08 nM, R squared: 0.984 (of [ 123 I]Italia), IC 50 : 1.36 nM, 95%CI: 0.5 nM −3.67 nM, R squared: 0.899 of [ 123 I]Italia_B), IC50: 2.96 nM, 95%CI: 1.1 nM-7.9 nM, R 2 : 0.970 (of racemic mix.). B ) Cell fractionation of [ 123 I]Italia_A in PSN-1 cells: western blot. C) Cell fractionation of [ 123 I]Italia_A in different cell lines. In membrane bound fraction. D) Cytoplasm soluble fraction. E) Chromatin soluble fraction. F) Nuclear soluble fraction.

Article Snippet: Human pancreatic adenocarcinoma cells (PSN-1), and human prostate cancer cells (PC-3) were purchased from ATCC; the murine breast cancer cell line 4T1 was a kind gift from prof. Nicola Sibson, Department of Oncology, University of Oxford.

Techniques: Cell Fractionation, Western Blot, Membrane

Journal: bioRxiv

Article Title: [ 123 I]Italia: A PARP-Directed Auger Electron-Emitting Agent for Targeted Radionuclide Therapy of Cancer

doi: 10.64898/2026.03.13.711622

Figure Lengend Snippet: A) Clonogenic survival of PSN-1 and PARP1 knock out cells (PSN-1 PARP1−/− ) after exposure of cells for 1h to [ 123 I]Italia_rac, and the separated enantiomers of [ 123 I]Italia_A or _B (0-500 kBq in 2 mL of growth medium). B) Clonogenic survival of various cell lines after exposure of cells for 1h to [ 123 I]Italia_A (0-500 kBq in 2mL of growth medium).

Article Snippet: Human pancreatic adenocarcinoma cells (PSN-1), and human prostate cancer cells (PC-3) were purchased from ATCC; the murine breast cancer cell line 4T1 was a kind gift from prof. Nicola Sibson, Department of Oncology, University of Oxford.

Techniques: Knock-Out

Journal: Frontiers in Oncology

Article Title: The effect of deuterated PLK1 inhibitor on its safety and efficacy in vivo

doi: 10.3389/fonc.2025.1510052

Figure Lengend Snippet: IC 50 values of PR00012 and NMS-P937 against human pancreatic cancer cell lines.

Article Snippet: For in vivo PK/PD studies, a PSN1 tumor model was established in female M-NSG (NOD.Cg- Prkdc scid Il2rg em1Smoc ) mice, which are severely immunodeficient mice lacking the interleukin 2 receptor gamma chain on a NOD.Cg- Prkdc scid background, at Shanghai Model Organisms (Shanghai, China).

Techniques:

Journal: Frontiers in Oncology

Article Title: The effect of deuterated PLK1 inhibitor on its safety and efficacy in vivo

doi: 10.3389/fonc.2025.1510052

Figure Lengend Snippet: Pharmacokinetics of PR00012 and NMS-P937 in PSN1 tumor CDX model using M-NSG mice. The tumor-bearing M-NSG mice were dosed with PR00012 or NMS-P937 at 60 mg/kg, 30 mg/kg, or 15 mg/kg. Blood samples were collected at seven time points. Compound concentration in the blood were determined and theT1/2 was calculated.

Article Snippet: For in vivo PK/PD studies, a PSN1 tumor model was established in female M-NSG (NOD.Cg- Prkdc scid Il2rg em1Smoc ) mice, which are severely immunodeficient mice lacking the interleukin 2 receptor gamma chain on a NOD.Cg- Prkdc scid background, at Shanghai Model Organisms (Shanghai, China).

Techniques: Drug discovery, Concentration Assay