328546-96-9

Upstream product

• 51616-10-5 4-(2-bromoethoxy)benzoyl chloride 
• 328546-66-3 9-amino-1,2,3,4-tetrahydro-5H-benzo[e][1,4]diazepin-5-one 
• 1567375-95-4 2-(4-(2-bromoethoxy)phenyl)-5,6-dihydro-imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one 
• 2386-52-9 silver methanesulfonate 

Downstream Products

• 1567375-87-4 [18F]-FTT 

Relevant academic research and scientific papers

RADIOLABELED TRACERS FOR POLY (ADP-RIBOSE) POLYMERASE-1 (PARP-1), METHODS AND USES THEREFOR

Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatr

Synthesis, [18F] radiolabeling, and evaluation of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors for in vivo imaging of PARP-1 using positron emission tomography

Imaging of poly (ADP-ribose) polymerase-1 (PARP-1) expression in vivo is a potentially powerful tool for developing PARP-1 inhibitors for drug discovery and patient care. We have synthesized several derivatives of benzimidazole carboxamide as PARP-1 inhibitors, which can be 18F-labeled easily for positron emission tomographic (PET) imaging. Of the compounds synthesized, 12 had the highest inhibition potency for PARP-1 (IC50 = 6.3 nM). [ 18F]12 was synthesized under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET studies using [ 18F]12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [18F]12 in the tumor that was blocked by olaparib, suggesting that the uptake of [18F]12 in the tumor is specific to PARP-1 expression.