FAP Ligand

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).

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.

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.

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.

DOTAGA.Glu.(FAPi) 2 is a FAPI homodimer in which a central glutamic acid (Glu) linker connects FAPI and a chelator. Radiolabeled with gallium-⁶⁸, lutetium-¹⁷⁷ or terbium-¹⁶¹, DOTAGA.Glu.(FAPi) 2 is applicable to FAP-positive cancer PET imaging studies. DOTAGA.Glu.(FAPi) 2 is suitable for research related to prostate adenocarcinoma and recurrent glioblastoma multiforme.

DOTA-ALB-01 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-01 labeled with ⁶⁸Ga or ¹⁷⁷Lu has a high FAP-binding affinity and enhanced tumor uptake and retention. DOTA-ALB-01 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers.

FAPI-JNU is a molecule targeting fibroblast activation protein (FAP). FAPI-JNU specifically binds to FAP highly expressed in the tumor microenvironment, and uses radionuclides [⁶⁸Ga]Ga or [¹⁷⁷Lu]Lu to achieve tumor imaging diagnosis. [177Lu]Lu−FAPI−JNU can effectively target and inhibit tumor growth in tumor-bearing mice. FAPI-JNU is promising for research of FAP-positive tumors (such as various solid tumors).

FAPI-FUSCC-07 is a targeted probe for fibroblast activation protein (FAP), exhibiting high affinity binding to FAP for applications in molecular imaging, tumor diagnosis, and radiotherapy.

NOTA-SP2A-FAPT is a fibroblast activation protein (FAP) ligand. NOTA-SP2A-FAPT can be adiolabeled and exhibits rapid renal excretion with fast kidney tissue clearance, accumulates rapidly in and retains high levels in FAP-positive tumor xenografts to enable clear tumor visualization. NOTA-SP2A-FAPT can be used as a tracer of cancer.

FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a K_d of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.

FAP Ligand 3 is a FAP ligand with a K_i value of 0.092 nM. FAP Ligand 3 acts as a tumor-retaining agent and serves as a FAP-targeted positron emission tomography (PET) tracer for tumor imaging. FAP Ligand 3 is applicable to studies related to glioma.