FAPI-04

Theranostic ligand for FAP. DOTA (Tetraxetan 2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]) chelating agent for metallic ions (177Lu and 68Ga for example) used in PET imaging. Gallium Ga 68-DOTA-FAPI-04 is a radioconjugate composed of FAPI-04, a quinoline-based fibroblast activation protein (FAP)-targeted tracer belonging to the group of FAP inhibitors (FAPi), conjugated, through the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), to the radioisotope gallium Ga 68

General

Type : Piperazine,Quinoline,PET probe,Carboxamide,tert-Butyl,tert-Butyloxycarbonyl

Chemical_Nomenclature : DOTA (S)-N-(2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)-6-(3-(4-tertbutoxycarbonyl-piperazin-1-yl)-1-propoxy)quinoline-4-carboxamide || 2-[4,7-bis(carboxymethyl)-10-[2-[4-[3-[4-[[2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]carbamoyl]quinolin-6-yl]oxypropyl]piperazin-1-yl]-2-oxoethyl]-1,4,7,10-tetrazacyclododec-1-yl]acetic acid

Canonical SMILES : C1CN(CCN1CCCOC3=CC2=C(C=CN=C2C=C3)C(=O)NCC(=O)N4CC(CC4C#N)(F)F)C(=O)CN5CCN(CCN(CCN(CC5)CC(=O)O)CC(=O)O)CC(=O)O || C1CN(CCN1CCCOC2=CC3=C(C=CN=C3C=C2)C(=O)NCC(=O)N4CC(CC4C#N)(F)F)C(=O)CN5CCN(CCN(CCN(CC5)CC(=O)O)CC(=O)O)CC(=O)O

InChI : InChI=1S\/C40H54F2N10O10\/c41-40(42)21-29(22-43)52(28-40)34(53)23-45-39(61)31-4-5-44-33-3-2-30(20-32(31)33)62-19-1-6-46-15-17-51(18-16-46)35(54)24-47-7-9-48(25-36(55)56)11-13-50(27-38(59)60)14-12-49(10-8-47)26-37(57)58\/h2-5,20,29H,1,6-19,21,23-28H2,(H,45,61)(H,55,56)(H,57,58)(H,59,60) || InChI=1S\/C40H54F2N10O10\/c41-40(42)21-29(22-43)52(28-40)34(53)23-45-39(61)31-4-5-44-33-3-2-30(20-32(31)33)62-19-1-6-46-15-17-51(18-16-46)35(54)24-47-7-9-48(25-36(55)56)11-13-50(27-38(59)60)14-12-49(10-8-47)26-37(57)58\/h2-5,20,29H,1,6-19,21,23-28H2,(H,45,61)(H,55,56)(H,57,58)(H,59,60)\/t29-\/m0\/s1

InChIKey : ICWDAESAANBIGG-UHFFFAOYSA-N || ICWDAESAANBIGG-LJAQVGFWSA-N

Other name(s) : ZZ7Stn2lbb,Gallium-68-fapi-04,68Ga-Fapi-04,(68Ga)-DOTA-fapi-04,FAPI-04 Ga-68,SCHEMBL21257058


MW : 872.91

Formula : C40H54F2N10O10

CAS_number :

PubChem : 155907829, 138454803

UniChem : ICWDAESAANBIGG-UHFFFAOYSA-N || ICWDAESAANBIGG-LJAQVGFWSA-N

IUPHAR :

Wikipedia :

Target

Families : FAPI-04 ligand of proteins in family: DPP4N_Peptidase_S9

Stucture :

Protein : human-FAP

References (3)

Title : Molecular Imaging of Fibroblast Activity After Myocardial Infarction Using a (68)Ga-Labeled Fibroblast Activation Protein Inhibitor, FAPI-04 - Varasteh_2019_J.Nucl.Med_60_1743
Author(s) : Varasteh Z , Mohanta S , Robu S , Braeuer M , Li Y , Omidvari N , Topping G , Sun T , Nekolla SG , Richter A , Weber C , Habenicht A , Haberkorn UA , Weber WA
Ref : J Nucl Med , 60 :1743 , 2019
Abstract : Varasteh_2019_J.Nucl.Med_60_1743
ESTHER : Varasteh_2019_J.Nucl.Med_60_1743
PubMedSearch : Varasteh_2019_J.Nucl.Med_60_1743
PubMedID: 31405922

Title : A Tumor-Imaging Method Targeting Cancer-Associated Fibroblasts - Loktev_2018_J.Nucl.Med_59_1423
Author(s) : Loktev A , Lindner T , Mier W , Debus J , Altmann A , Jager D , Giesel F , Kratochwil C , Barthe P , Roumestand C , Haberkorn U
Ref : J Nucl Med , 59 :1423 , 2018
Abstract : Loktev_2018_J.Nucl.Med_59_1423
ESTHER : Loktev_2018_J.Nucl.Med_59_1423
PubMedSearch : Loktev_2018_J.Nucl.Med_59_1423
PubMedID: 29626120
Gene_locus related to this paper: human-FAP

Title : Development of Quinoline-Based Theranostic Ligands for the Targeting of Fibroblast Activation Protein - Lindner_2018_J.Nucl.Med_59_1415
Author(s) : Lindner T , Loktev A , Altmann A , Giesel F , Kratochwil C , Debus J , Jager D , Mier W , Haberkorn U
Ref : J Nucl Med , 59 :1415 , 2018
Abstract : Lindner_2018_J.Nucl.Med_59_1415
ESTHER : Lindner_2018_J.Nucl.Med_59_1415
PubMedSearch : Lindner_2018_J.Nucl.Med_59_1415
PubMedID: 29626119
Gene_locus related to this paper: human-FAP