Peptide Conjugates

DOTA-WC8 is a HER2-targeting peptide probe with a K_D of 61.20 nM. ⁶⁸Ga-labeled DOTA-WC8 serves as a PET imaging agent for the specific identification of HER2-positive breast cancer. DOTA-WC8 is applicable to breast cancer-related research.

PSMA-N5 (Compound 15) is a PSMA ligand with a K_i value of 0.71 nM. PSMA-N5 acts as a PET radiotracer for prostate cancer imaging. PSMA-N5 is applicable to the research of prostate cancer and other related cancers.

JMV 7490 is a highly potent and highly hydrophilic neurotensin receptor NTS₁ probe that can be successfully labeled with ⁶⁸Ga and ¹¹¹In. JMV 7490 acts as an efflux inhibitor to reduce its efflux in NTS₁-positive cancer cells; it also serves as an internalization inducer and is efficiently and continuously internalized by NTS₁-positive cancer cells. ¹¹¹In-radiolabeled JMV 7490 shows persistent uptake in NTS₁-positive xenografts in nude mice, but no significant uptake in NTS₁-negative xenografts. JMV 7490 can be used for in vivo tracer applications of NTS1-positive tumors and supports related research on colorectal cancer.

DOTA-C1-FAP-2286 is a cysteic acid-modified fibroblast activation protein (FAP)-targeting radioligand. DOTA-C1-FAP-2286 binds competitively to FAP with an IC₅₀ of 127.64 nM. DOTA-C1-FAP-2286 is targeted accumulation in FAP-expressing cells and exhibits accelerated renal clearance. DOTA-C1-FAP-2286 can be used as a PET/CT tracer in cancer.

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.

JR11-PEG3-DOTA-PSMA-03 (Compound 2) is an RDC-related compound containing the chelating agent DOTA (HY-W053583), the JR11 peptide (SSTR2 antagonist), and the PSMA ligand. JR11-PEG3-DOTA-PSMA-03 shows SSTR2-binding affinities and PSMA-binding affinities, with IC₅₀ s of 94.0 nM, 81.8 nM, respectively. JR11-PEG3-DOTA-PSMA-03 can be radiolabeled with [⁶⁸Ga]. [⁶⁸Ga] radiolabeled JR11-PEG3-DOTA-PSMA-03 can be used in diagnostic studies of neuroendocrine differentiated prostate cancer.

NOTA-RHAU18 is a conjugate of the chelator NOTA and the peptide RHAU18. NOTA-RHAU18 can be used to synthesize the radiolabeled peptide probe [¹⁸F]AlF-NOTA-RHAU18. [¹⁸F]AlF-NOTA-RHAU18 targets mitochondrial DNA G4. [¹⁸F]AlF-NOTA-RHAU18 can be used to visualize and detect solid tumors in homozygous mice. [¹⁸F]AlF-NOTA-RHAU18 can also be used in PET imaging studies.

JR11-PEG3-HBED-CC-PSMA-03 (Compound 1) is an RDC-related compound containing the chelating agent HBED-CC, the JR11 peptide (SSTR2 antagonist), and the PSMA ligand. JR11-PEG3-HBED-CC-PSMA-03 shows SSTR2-binding affinities and PSMA-binding affinities, with IC₅₀ s of 59.2 nM, 57.0 nM, respectively. JR11-PEG3-HBED-CC-PSMA-03 can be radiolabeled with [⁶⁸Ga]. [⁶⁸Ga] radiolabeled JR11-PEG3-HBED-CC-PSMA-03 can be used in diagnostic studies of neuroendocrine differentiated prostate cancer.

Alizulatide vixocianine is a polypeptide that can be discovered through polypeptide screening. Polypeptide screening is a research tool mainly based on immunoassay methods to identify active polypeptides. It can be applied to protein interaction, functional analysis, antigenic epitope screening, especially in the fields of active molecule research and development.

DOTA-Bn-CA-170 is a molecular probe targeting the VISTA protein, with a K_d value of 0.124 nM. DOTA-Bn-CA-170 is formed by covalently linking the p-SCN-Bn-DOTA ligand with CA-170 (HY-101093). DOTA-Bn-CA-170 labeled with [⁶⁸Ga]Ga successfully achieves specific and high-contrast PET imaging of VISTA expression in various tumor-bearing mouse models. DOTA-Bn-CA-170 can be used for the study of VISTA-targeted immunotherapy.

DOTA-BP1 is a DOTA-modified BP1 (BCMA-targeting peptide). DOTA-BP1 can be radiolabeled with [⁶⁸Ga]Ga to produce a BCMA-targeting PET tracer. DOTA-BP1 can be used in the research of detecting BCMA in multiple myeloma.

DOTA-CA-170 is a DOTA-modified VISTA targeting agent CA-170. DOTA-CA-170 can be radiolabeled. DOTA-CA-170 can be used in the research of visualizing and distinguishing VISTA expression.

DOTA-FAPT is a novel targeting FAP tracer. DOTA-FAPT can be radiolabeled with gallium-68 and lutetium-177. DOTA-FAPT can be used for PET imaging studies of cancer-associated fibroblasts.

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.

NOTA-SFCVHEM can be activated by CTB. NOTA-SFCVHEM can be used to prepare PET tracer. NOTA-SFCVHEM has good stability, low toxicity, high tumor selectivity, and low liver accumulation.

AAZTA-NI-PSMA-093 is a bispecific agent targeting prostate-specific membrane antigen (PSMA) with an IC₅₀ value for PSMA of 87.48 nM. AAZTA-NI-PSMA-093 has a PSMA targeting module and an oxygen-sensitivity module (hypoxia-sensitive NI-moiety). AAZTA-NI-PSMA-093 can utilize the PSMA targeting property as a "navigation system" to efficiently concentrate the entire molecule within prostate cancer cells, and once the cells are in an oxygen-deficient state, the molecule will irreversibly capture and remain in the oxygen-deficient cells, achieving "secondary enrichment". AAZTA-NI-PSMA-093 can be labeled with ⁶⁸Ga and ¹⁷⁷Lu, and has high accumulation and rapid clearance characteristics in mouse models. AAZTA-NI-PSMA-093 can be used for the study of prostate cancer.

Lipo-PtIV-R8K is a nuclear targeting peptide containing R8K. Lipo-PtIV-R8K is a lipid PtIV prodrug amphiphilic molecule that can self assemble to form nanoparticles. Lipo-PtIV-R8K can be used in the research of cancer such as breast cancer.

DOTA-TMVP1446 is a VEGFR-3 targeting peptide. DOTA-TMVP1446 labeled with ⁶⁸Ga accurately detectes the status of lymph node metastasis, even in micrometastatic tumors, in the B16-F10 tumor mice model. DOTA-TMVP1446 can be used as a radiotracer for cancer-metastatic sentinel lymph nodes (m-SLN) imaging.

Talovirtide is a peptide containing L-valyl.

Tezuvotide tetraxetan is an antineoplastic peptide.