PNT6555

PNT6555 and its gallium (natGa-PNT6555) and lutetium (natLu-PNT6555) chelates showed potent activity in FAP inhibition assays using human, mouse, and rat sources of FAP(ubiquitous chelator DOTA 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) linked to analogue of peptide. CID 168489455 is the Lutetium chelate, CID 168489454 is the Gallium chelate

General

Type : PET probe,Peptide

Chemical_Nomenclature : 2-[4-[2-[[4-[[(2R)-1-[(2R)-2-boronopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamoyl]phenyl]methylamino]-2-oxoethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid

Canonical SMILES : (C1CCCN1C(=O)C(C)NC(=O)C2=CC=C(C=C2)CNC(=O)CN3CCN(CCN(CCN(CC3)CC(=O)O)CC(=O)O)CC(=O)O)(O)O

InChI : InChI=1S\/C31H48BN7O11\/c1-22(31(48)39-8-2-3-25(39)32(49)50)34-30(47)24-6-4-23(5-7-24)17-33-26(40)18-35-9-11-36(19-27(41)42)13-15-38(21-29(45)46)16-14-37(12-10-35)20-28(43)44\/h4-7,22,25,49-50H,2-3,8-21H2,1H3,(H,33,40)(H,34,47)(H,41,42)(H,43,44)(H,45,46)\/t22-,25+\/m1\/s1

InChIKey : PTVMRWQEZPTMFA-RDGATRHJSA-N

Other name(s) : DOTA-AmBz-d-Ala-boroPro,DOTA-aminomethylbenzoyl-d-Ala-boroPro,DOTA-aminomethyl-Bz-D-Ala-boroPro,BDBM609722,BDBM609773,US11707539, Compound 6555LU,DOTA- aminomethyl-Bz- D-Ala-boroPro,US11707539, Compound 6555,BDBM609772,US11707539, Compound 6555GA


MW : 705.6

Formula : C31H48BN7O11

CAS_number :

PubChem : 168489413, 168489455, 168489454

UniChem : PTVMRWQEZPTMFA-RDGATRHJSA-N

IUPHAR :

Wikipedia :

Target

Families : PNT6555 ligand of proteins in family: DPP4N_Peptidase_S9

Stucture :

Protein : human-FAP

References (3)

Title : Preclinical Development of PNT6555, a Boronic Acid-Based, Fibroblast Activation Protein-alpha (FAP)-Targeted Radiotheranostic for Imaging and Treatment of FAP-Positive Tumors - Poplawski_2023_J.Nucl.Med__
Author(s) : Poplawski SE , Hallett RM , Dornan MH , Novakowski KE , Pan S , Belanger AP , Nguyen QD , Wu W , Felten AE , Liu Y , Ahn SH , Hergott VS , Jones B , Lai JH , McCann JAB , Bachovchin WW
Ref : J Nucl Med , : , 2023
Abstract : Poplawski_2023_J.Nucl.Med__
ESTHER : Poplawski_2023_J.Nucl.Med__
PubMedSearch : Poplawski_2023_J.Nucl.Med__
PubMedID: 38050111

Title : Synthesis and Preclinical Evaluation of Novel (68)Ga-Labeled (R)-Pyrrolidin-2-yl-boronic Acid-Based PET Tracers for Fibroblast Activation Protein-Targeted Cancer Imaging - Bendre_2023_Pharmaceuticals.(Basel)_16_798
Author(s) : Bendre S , Kuo HT , Merkens H , Zhang Z , Wong A , Benard F , Lin KS
Ref : Pharmaceuticals (Basel) , 16 :798 , 2023
Abstract : Bendre_2023_Pharmaceuticals.(Basel)_16_798
ESTHER : Bendre_2023_Pharmaceuticals.(Basel)_16_798
PubMedSearch : Bendre_2023_Pharmaceuticals.(Basel)_16_798
PubMedID: 37375746

Title : Fibroblast activation protein-targeted radionuclide therapy: background, opportunities, and challenges of first (pre)clinical studies - Prive_2023_Eur.J.Nucl.Med.Mol.Imaging_50_1906
Author(s) : Prive BM , Boussihmad MA , Timmermans B , van Gemert WA , Peters SMB , Derks YHW , van Lith SAM , Mehra N , Nagarajah J , Heskamp S , Westdorp H
Ref : Eur J Nucl Med Mol Imaging , 50 :1906 , 2023
Abstract : Prive_2023_Eur.J.Nucl.Med.Mol.Imaging_50_1906
ESTHER : Prive_2023_Eur.J.Nucl.Med.Mol.Imaging_50_1906
PubMedSearch : Prive_2023_Eur.J.Nucl.Med.Mol.Imaging_50_1906
PubMedID: 36813980