FAP

AZD2389 is a potent and orally active FAP inhibitor. AZD2389 can be used for the study of metabolic dysfunction-associated steatohepatitis.

FAP-IN-2 is an isonitrile-containing fibroblast activation protein (FAP) inhibitor. FAP-IN-2 can be labeled with technetium-99m (^99mTc) for targeted tumor SPECT imaging.

NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI can be used as a probe for FAP-targeted tumour imaging. NOTA-FAPI has good tumour detection efficacy and excellent imaging quality.

3BP-4089 TFA is a highly efficient fibroblast activation protein (FAP) targeting peptide. 3BP-4089 TFA is often conjugated with radionuclides for tumor diagnosis and research.

DOTA.SA.FAPi TFA is a selective FAP inhibitor with an IC₅₀ value of 0.9 nM against FAP. DOTA.SA.FAPi TFA forms stable complexes with ⁶⁸Ga and serves as a PET radiotracer for preclinical imaging of FAP-expressing tumors. DOTA.SA.FAPi TFA can be used in the research of colorectal adenocarcinoma and various other cancers.

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

FAPI-34 is a SPECT imaging agent targeting FAP. FAPI-34 specifically binds to FAP, is highly internalized by FAP-expressing cells, accumulates in FAP-expressing tumor lesions, and shows low uptake in normal tissues except the kidneys. FAPI-34 is applicable for tumor-related research.

PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors.

DOTAGA.(SA.FAPi)2 TFA is a potent dimeric fibroblast-activation protein inhibitor (FAPi). DOTAGA.(SA.FAPi)2 TFA has the potential for cancer diagnosis research.

FAPI-800CW is a near-infrared (NIR) fluorescent-labeled fibroblast activation protein (FAP) inhibitor. FAPI-800CW shows specific uptake in inflamed paws in collagen-induced arthritis (CIA) model mice. FAPI-800CW can be used for in vivo molecular imaging of FAP expression in inflammatory diseases such as rheumatoid arthritis (RA) to monitor joint inflammation and disease activity.

FAP-IN-2 TFA is an isonitrile-containing fibroblast activation protein (FAP) inhibitor. FAP-IN-2 TFA can be labeled with technetium-99m (^99mTc) for targeted tumor SPECT imaging.

OncoFAP-GlyPro-MMAE is a FAP small molecule-drug conjugate (SMDC) with an IC₅₀ of 0.49  nM. OncoFAP-GlyPro-MMAE consists of a FAP Ligand OncoFAP (HY-145938), a Tubulin inhibitor (MMAE) (HY-15162) and a linker. OncoFAP-GlyPro-MMAE can be used for cancers like renal cancer research.

DOTAGA-FAP-2286-ALB is a derivative of Rofapitide tetraxetan (HY-147057). DOTAGA-FAP-2286-ALB is a selective fibroblast activation protein (FAP) inhibitor with an IC₅₀ value of 67.5 nM. DOTAGA-FAP-2286-ALB enhances tumor retention via albumin interaction, prolonging blood circulation and improving radiometal complex stability (e.g., with 111In and 225Ac). DOTAGA-FAP-2286-ALB is promising for research of radionuclide therapy (TRT) of FAP-positive solid tumors.

NH2-UAMC1110 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 is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose-response, and has been used for tumor diagnosis. NH2-UAMC1110 introduces an active amino group into its structure, enabling it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.), thereby synthesizing molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 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 processes. Its key activity is high targeting and high affinity, and its core function is to be coupled with bifunctional chelators (such as DOTA, DATA5m) as a targeting module. NH2-UAMC1110 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.

DOTA-ALB-02 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-02 labeled with ¹⁷⁷Lu has a high FAP-binding affinity and enhanced tumor uptake and retention with a significant tumor/nontarget ratio. DOTA-ALB-02 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers.

Zilganersen (ION373) sodium is a gapmer antisense oligonucleotide targeting glial fibrillary acidic protein (GFAP). Zilganersen sodium reduces excess glial fibrillary acidic protein produced by disease-causing variants in the GFAP gene and inhibits synthesis of GFAP. Zilganersen sodium can be used for the research of Alexander disease.

OMTX005 (OMTX705 antibody) is a humanized anti-FAP IgG1 monoclonal antibody that specifically binds to human (EC₅₀: 0.33 nM)/mouse (EC₅₀: 0.14 nM) FAP proteins and FAP-positive cells. OMTX005 exhibits no cytotoxicity when used alone and fails to induce an increase in caspase 3/7 activity in relevant cells. OMTX005 can be used to synthesize the ADC molecule OMTX705 for tumor research.

SID 125240931 is a fluorogen activating proteins (FAPs) modulator. SID 125240931 interferes with the binding between fluorogens and FAP.

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

FAPI-2 is a quinoline-based fibroblast activation protein (FAP)-targeting ligand that can be labeled as ⁶⁸Ga-FAPI-2 and used as a PET tracer for cancer diagnosis. FAPI-2 has advantages such as fast tracer kinetics, no need for fasting preparation, and being unaffected by blood glucose.