Rofapitide tetraxetan

Rofapitide tetraxetan (FAP-2286) is a potent and selective FAP-binding peptide with a mean IC50 value of 2.7 nM for binding to FAP. Rofapitide tetraxetan can be labeled with radionuclides for diagnostic applications. Rofapitide tetraxetan has antitumor activity[1].

Product Specifications

CAS Number

[2581741-18-4]

Product Name Alternative

FAP-2286

UNSPSC

12352005

Target

FAP

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/fap-2286.html

Purity

99.54

Solubility

DMSO : ≥ 50 mg/mL|H2O : ≥ 100 mg/mL

Smiles

O=C(N1[C@@](C(N[C@@](C(N[C@H](C(N[C@H](C2=O)CC3=CC=CC=C3)=O)CCC(N)=O)=O)([H])[C@H](O)C)=O)([H])CCC1)[C@@](CCC4)([H])N4C([C@H](CSCC5=CC(CSCCNC(CN(CCN(CC6)CC(O)=O)CCN(CCN6CC(O)=O)CC(O)=O)=O)=CC(CSC[C@H](N2)C(O)=O)=C5)NC(CCCCC)=O)=O

Molecular Formula

C67H99N13O18S3

Molecular Weight

1470.77

References & Citations

[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.