FAP

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.

FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted tracer. Use radioactivity FAPI-46 labeled with ⁶⁸Ga or ¹⁷⁷Lu can be used for tumor imaging in a variety of cancers and has higher tumor uptake rates and longer tumor accumulation.

FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. ⁶⁸Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.

UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC₅₀ of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC₅₀ of 1.8 μM.

Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC).

Cys-FAP targeting peptide for FXX489 TFA is the polypeptide part of Unlabeled FXX489 (HY-P10944). Unlabeled FXX489 is a fibroblast activation protein (FAP)-targeting ligand.

L-Ala-BPA is a boron delivery agent. L-Ala-BPA is transported into tumor cells via PEPT1/2 and LAT-1 (SLC7A5) pathways and is rapidly cleaved systemically by endogenous proteases including FAP to yield L-BPA (HY-W087830). L-Ala-BPA shows antitumor activity and can be used for the research of Boron Neutron Capture Therapy (BNCT).

GFAP/NF-κB/APOE/NLRP3-IN-1 is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC₅₀ of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC₅₀ of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ_1-42 aggregation with an IC₅₀ of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma.

Ac-Gly-BoroPro is a selective FAP inhibitor with a K_i of 23 nM.

Suc-Gly-Pro-AMC is a fluorescent substrate. Suc-Gly-Pro-AMC is a fibroblast activation protein (FAP) specific substrate. Suc-Gly-Pro-AMC reacts with recombinant porcine prolyl oligopeptidase. Suc-Gly-Pro-AMC can be used to study the activity of FAP, prolyl endopeptidase (PREP). Suc-Gly-Pro-AMC is used in glioma research.

FAPI-74 is a PET (positron emission tomography) tracer targeting the fibroblast activation protein (FAP). FAPI-74 can be used for FAP-positive tumor research.

NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis.

Anti-Mouse FAP Antibody (73.3) is an anti-mouse FAP IgG1 monoclonal antibody. Anti-Mouse FAP Antibody (73.3) can be used to accurately detect the expression and localization of FAP protein in mice. Anti-Mouse FAP Antibody (73.3) can be used for research on cancer.

OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.

Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with ⁶⁸Ga and ¹⁷⁷Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC).

ARI-3144 is an excellent and specific substrate for fibroblast activation protein (FAP). ARI-3144 is usually coupled with the fluorophore 7-Amino-4-methylcoumarin (HY-D0027) (AMC) for detection and quantification of FAP.

FAPI-mFS is an irreversible fibroblast activation protein (FAP) inhibitor, that enhances the uptake and retention time in cancer cells through its covalent binding property for FAP. FAPI-mFS can be used for cancer imaging the therapy, when labeled with radioactive 68Ga or 177Lu. FAPI-mFS can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

3BP-3940 is a highly potent and selective peptide inhibitor of FAP that targets cancer-associated fibroblasts (CAFs) in the tumor microenvironment. 3BP-3940 can be labeled with radionuclides (such as Ga-68) for precise tumor imaging or Lu-177 for the development of targeted anticancer technologies. 3BP-3940 accumulates in tumor lesions and can be used to diagnose and inhibit various solid cancers and CAFs-related diseases.

ARI-3099 is an oral fibroblast activation protein (FAP) inhibitor. ARI-3099 specifically inhibits the proteolytic activity of FAP and blocks the cleavage of human FGF-21 between residues P171 and S172. ARI-3099 extends the half-life of circulating human FGF-21 in mice. ARI-3099 can be used in the research of type 2 diabetes and metabolic disorders.

FT-FAPI-12_9 is a FAP ligand that can be used to synthesize FAPI-46, a radiotracer targeting FAP.