DOTAGA-Glu-FAPi2
General
Type : PET probe, Tetrazacyclododec, Pyrrolidine, Quinoline, Piperazine
Chemical_Nomenclature : 5-[[(2S)-1,5-bis[4-[4-[[2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]carbamoyl]quinolin-6-yl]oxybutylamino]-1,5-dioxopentan-2-yl]amino]-5-oxo-2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]pentanoic acid
Canonical SMILES : C1CN(CCN(CCN(CCN1CC(=O)O)CC(=O)O)C(CCC(=O)N[C@@H](CCC(=O)NCCCCOC2=CC3=C(C=CN=C3C=C2)C(=O)NCC(=O)N4CC(C[C@H]4C#N)(F)F)C(=O)NCCCCOC5=CC6=C(C=CN=C6C=C5)C(=O)NCC(=O)N7CC(C[C@H]7C#N)(F)F)C(=O)O)CC(=O)O
InChI : InChI=1S\/C66H81F4N15O17\/c67-65(68)31-42(33-71)84(40-65)56(88)35-77-61(96)46-13-17-73-50-7-5-44(29-48(46)50)101-27-3-1-15-75-54(86)11-9-52(79-55(87)12-10-53(64(99)100)83-25-23-81(38-59(92)93)21-19-80(37-58(90)91)20-22-82(24-26-83)39-60(94)95)63(98)76-16-2-4-28-102-45-6-8-51-49(30-45)47(14-18-74-51)62(97)78-36-57(89)85-41-66(69,70)32-43(85)34-72\/h5-8,13-14,17-18,29-30,42-43,52-53H,1-4,9-12,15-16,19-28,31-32,35-41H2,(H,75,86)(H,76,98)(H,77,96)(H,78,97)(H,79,87)(H,90,91)(H,92,93)(H,94,95)(H,99,100)\/t42-,43-,52-,53?\/m0\/s1
InChIKey : QZWCXNGVONQIBK-OKNCFRBBSA-N
Other name(s) : DOTAGA-Glu(FAPi)-FAPi-amide || SCHEMBL30069167 || EX-A15970
MW : 1432.4
Formula : C66H81F4N15O17
CAS_number : 2882922-68-9
PubChem : 171774490
UniChem : QZWCXNGVONQIBK-OKNCFRBBSA-N
Target
Families : DOTAGA-Glu-FAPi2 ligand of proteins in family
DPP4N_Peptidase_S9
Protein :
human-FAP
References (9)
| Title : In vitro kinetic profiling by enzymatic approaches to select FAPIs with a long residence time - Verhulst_2026_Eur.J.Med.Chem_304_118494 |
| Author(s) : Verhulst E , Brzeminski P , de Groot A , Wals JW , Michiels R , Fabisiak A , Thys J , Grintsevich S , Van Rymenant Y , Peeters S , Lambregts S , Sim Y , Verstraete R , Van Wielendaele P , Berg M , Elvas F , Van Ostade X , Rosch F , Lambeir AM , De Winter H , Van der Veken P , De Meester I |
| Ref : Eur Journal of Medicinal Chemistry , 304 :118494 , 2026 |
| Abstract : |
| PubMedSearch : Verhulst_2026_Eur.J.Med.Chem_304_118494 |
| PubMedID: 41455278 |
| Gene_locus related to this paper: human-FAP |
| Title : FAP-Inhibitor Homodimers with Engineered Linker-Spacer Units: Toward Optimized Radiopharmaceuticals - Kumar_2026_ACS.Omega_11_49001 |
| Author(s) : Kumar N , Martin M , Bilinska A , Menendez E , De Meester I , Roesch F , Rominger A , Gourni E |
| Ref : ACS Omega , 11 :49001 , 2026 |
| Abstract : |
| PubMedSearch : Kumar_2026_ACS.Omega_11_49001 |
| PubMedID: 42662658 |
| Title : Preclinical evaluation of DOTAGA.Glu.(FAPI)(2) and DO3A.Glu.(FAPI)(2) as theranostics with human dosimetry extrapolation to lutetium-177 and terbium-161 analogs - Bilinska_2026_Eur.J.Nucl.Med.Mol.Imaging_53_1887 |
| Author(s) : Bilinska A , Kumar N , Gnesin S , Lappchen T , Menendez E , Martin M , Rosch F , Rominger A , Gourni E |
| Ref : Eur J Nucl Med Mol Imaging , 53 :1887 , 2026 |
| Abstract : |
| PubMedSearch : Bilinska_2026_Eur.J.Nucl.Med.Mol.Imaging_53_1887 |
| PubMedID: 41105225 |
| Title : Molar Dose Optimization for Accurate Pharmacokinetic and Biodistribution Evaluation of FAP-Targeted Radiopharmaceuticals in a Mouse Syngeneic Tumor Model - Liu_2026_Mol.Pharm_23_1189 |
| Author(s) : Liu L , He S , Huang Z , Wang D , Zhou J , Yang J , Shi Y , Cheng Z , Cheng S , Zou S , Zhao J , Zhu X |
| Ref : Mol Pharm , 23 :1189 , 2026 |
| Abstract : |
| PubMedSearch : Liu_2026_Mol.Pharm_23_1189 |
| PubMedID: 41486728 |
| Title : Homomultimeric FAP Inhibitor-Based Radioligands for Cancer Theranostics: Design Principles, Structure-Function Relationships, and Preclinical Performance - Wu_2026_Molecules_31_2124 |
| Author(s) : Wu Z , Gourni E , Ballal S , Van der Veken P , Roesch F |
| Ref : Molecules , 31 : , 2026 |
| Abstract : |
| PubMedSearch : Wu_2026_Molecules_31_2124 |
| PubMedID: 42357520 |
| Title : Efficacy and Safety of [(177)Lu]Lu-DOTAGA.Glu.(FAPi)(2) Therapy in Patients with Sarcoma - Ballal_2025_J.Nucl.Med_66_1612 |
| Author(s) : Ballal S , Sakir M , Chandekar KR , Rastogi S , Yadav MP , Roesch F , Tripathi M , Martin M , Bal C |
| Ref : J Nucl Med , 66 :1612 , 2025 |
| Abstract : |
| PubMedSearch : Ballal_2025_J.Nucl.Med_66_1612 |
| PubMedID: 40841150 |
| Title : [(68)Ga]Ga-DOTAGA-Glu(FAPi)(2) Shows Enhanced Tumor Uptake and Theranostic Potential in Preclinical PET Imaging - Mortensen_2024_Diagnostics.(Basel)_14_ |
| Author(s) : Mortensen JVK , Mattiussi S , Hvass L , Lund EG , Shalgunov V , Roesch F , Battisti UM , Herth MM , Kjaer A |
| Ref : Diagnostics (Basel) , 14 : , 2024 |
| Abstract : |
| PubMedSearch : Mortensen_2024_Diagnostics.(Basel)_14_ |
| PubMedID: 39335703 |
| Title : [(177)Lu]Lu-DOTAGA.Glu.(FAPi)(2) Radionuclide Therapy: a New Treatment Option for Patients with Glioblastoma Multiforme - Ballal_2024_Nucl.Med.Mol.Imaging_58_32 |
| Author(s) : Ballal S , Yadav MP , Raju S , Roesch F , Martin M , Tripathi M , Bal C |
| Ref : Nucl Med Mol Imaging , 58 :32 , 2024 |
| Abstract : |
| PubMedSearch : Ballal_2024_Nucl.Med.Mol.Imaging_58_32 |
| PubMedID: 38261876 |
| Title : Novel Generation of FAP Inhibitor-Based Homodimers for Improved Application in Radiotheranostics - Martin_2023_Cancers.(Basel)_15_ |
| Author(s) : Martin M , Ballal S , Yadav MP , Bal C , Van Rymenant Y , De Loose J , Verhulst E , De Meester I , Van der Veken P , Roesch F |
| Ref : Cancers (Basel) , 15 : , 2023 |
| Abstract : |
| PubMedSearch : Martin_2023_Cancers.(Basel)_15_ |
| PubMedID: 36980775 |