FAP-2286 without DOTA chelator peptide

FAP-2286 without DOTA chelator peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Batch to batch variation of the purity

Hex-[Cys(tMeBn(AET))-PPTQFC]-OH

Hex-[Cys(tMeBn(AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH

7

95.46%

Synthetic

Powder

FAP-2286 is a novel compound designed to target the fibroblast activation protein (FAP), which is selectively expressed in the tumor microenvironment of many solid cancers but has limited expression in normal adult tissues. FAP-2286 consists of a FAP-binding cyclic peptide conjugated to a radionuclide chelator, enabling it to be used for both imaging and therapeutic purposes in cancer treatment. In preclinical studies, radiolabeled versions of FAP-2286 demonstrated high tumor uptake, prolonged retention, and significant antitumor activity in FAP-expressing tumors. This compound shows promise as a theranostic agent, with versions like 68Ga-FAP-2286 being used for imaging and 177Lu-FAP-2286 for therapeutic applications. It outperformed other FAP-targeting agents, such as FAPI-46, in terms of tumor retention and efficacy, supporting its potential for clinical development in treating FAP-positive tumors

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides

• Zboralski D, Hoehne A, Bredenbeck A, Schumann A, Nguyen M, Schneider E, Ungewiss J, Paschke M, Haase C, von Hacht JL, Kwan T, Lin KK, Lenore J, Harding TC, Xiao J, Simmons AD, Mohan AM, Beindorff N, Reineke U, Smerling C, Osterkamp F. 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. doi: 10.1007/s00259-022-05842-5. Epub 2022 May 24. PMID: 35608703; PMCID: PMC9399058.

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.