For research use only. Not for therapeutic Use.
FAP-2286 is a potent and selective FAP-binding peptide coupled to a radionuclide chelator with a mean IC50 value of 2.7 nM for binding to FAP. FAP-2286 can chelate radionuclides for imaging or therapeutic applications and has a strong effect on FAP-positive tumors. FAP-2286 can be used for FAP-positive tumor research[1].
FAP-2286 (0.1-30 nM, 1 h) reduces fuorophore-labeled competitor peptide bound to cells in human WI-38 fibroblast like fetal lung cell line[1].
FAP-2286 (5 nM, 1, 3, 8, 24, and 72 h) maintains long tumor retention and suppression in HEK-FAP cells[1].
FAP-2286 (30 MBq/nmol for intravenous injection) accumulated atably maintained in the tumors of HEK-FAP tumor-bearing mice[1].
| Catalog Number | I043667 |
| CAS Number | 2581741-18-4 |
| Synonyms | (5R,11S,17S,20S,23S,26S,29R)-23-(3-amino-3-oxopropyl)-26-benzyl-5-(hexanoylamino)-20-[(1R)-1-hydroxyethyl]-6,12,18,21,24,27-hexaoxo-35-[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]ethylsulfanylmethyl]-3,31-dithia-7,13,19,22,25,28-hexazatetracyclo[31.3.1.07,11.013,17]heptatriaconta-1(37),33,35-triene-29-carboxylic acid |
| Molecular Formula | C67H99N13O18S3 |
| Purity | ≥95% |
| InChI | InChI=1S/C67H99N13O18S3/c1-3-4-6-15-55(83)70-50-41-100-39-46-30-45(38-99-29-18-69-56(84)34-75-21-23-76(35-57(85)86)25-27-78(37-59(89)90)28-26-77(24-22-75)36-58(87)88)31-47(32-46)40-101-42-51(67(97)98)73-62(92)49(33-44-11-7-5-8-12-44)72-61(91)48(16-17-54(68)82)71-64(94)60(43(2)81)74-63(93)52-13-9-19-79(52)66(96)53-14-10-20-80(53)65(50)95/h5,7-8,11-12,30-32,43,48-53,60,81H,3-4,6,9-10,13-29,33-42H2,1-2H3,(H2,68,82)(H,69,84)(H,70,83)(H,71,94)(H,72,91)(H,73,92)(H,74,93)(H,85,86)(H,87,88)(H,89,90)(H,97,98)/t43-,48+,49+,50+,51+,52+,53+,60+/m1/s1 |
| InChIKey | UHKLVUPDBJFFBB-ZCDGVBLYSA-N |
| SMILES | CCCCCC(=O)NC1CSCC2=CC(=CC(=C2)CSCCNC(=O)CN3CCN(CCN(CCN(CC3)CC(=O)O)CC(=O)O)CC(=O)O)CSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C4CCCN4C(=O)C5CCCN5C1=O)C(C)O)CCC(=O)N)CC6=CC=CC=C6)C(=O)O |
| Reference | [1]. Dirk Zboralski, et al. Comparative Biodistribution and Radiotherapeutic Efficacy of the Fibroblast Activation Protein (FAP)–Targeting Agents FAP-2286 and FAPI-46. [2]. Richard P Baum, et al. Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using 177 Lu-FAP-2286: First-in-Humans Results. J Nucl Med. 2022 Mar;63(3):415-423. [3]. Zboralski D, Hoehne A, Bredenbeck A, et al. Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy. Eur J Nucl Med Mol Imaging. 2022;49(11):3651-3667. [4]. Pang Y, Zhao L, Meng T, et al. PET Imaging of Fibroblast Activation Protein in Various Types of Cancer Using 68Ga-FAP-2286: Comparison with 18F-FDG and 68Ga-FAPI-46 in a Single-Center, Prospective Study. J Nucl Med. 2023;64(3):386-394. [5]. Zboralski D, et al. Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy. Eur J Nucl Med Mol Imaging. 2022 Sep;49(11):3651-3667. |
