PSMA Ligand

PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that acts as a tumor retention agent, renal uptake reducer, imaging agent and antitumor agent, applicable in SPECT diagnostic imaging and radiotheranostics. PDI2 specifically binds to PSMA on prostate cancer cells, enters cells via clathrin-dependent endocytosis, and exhibits higher tumor retention rate and lower renal uptake level. PDI2 is applicable in research related to prostate cancer and castration-resistant metastatic prostate cancer.

PSMA-azide is a prostate-specific membrane antigen (PSMA) ligand. PSMA-azide inhibits PSMA-dependent NAAG (N-acetylaspartylglutamic acid) hydrolysis, with an IC₅₀ of 9 nM and a K_i of 1 nM. PSMA-azide contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups.

PNT2001 (LY4181530) is a potent prostate specific membrane antigen (PSMA) ligand with an IC₅₀ of 3.1 nM. PNT2001 can improve cellular internalization. 177Lu- and 225Ac-labeled PNT2001 can be used in prostate cancer research.

EC1169 is a cytotoxic maytansinoid conjugate that specifically binds to prostate-specific membrane antigen (PSMA). EC1169 precisely delivers the maytansinoid B hydrazide payload to PSMA-positive cells to exert antitumor activity. EC1169 only inhibits the growth of PSMA-positive cells but has no effect on PSMA-negative cells, and enables complete recovery in mice bearing PSMA-positive tumors. EC1169 exhibits safety with no body weight loss or major organ damage induced. EC1169 is used in studies of prostate cancer and other PSMA-expressing malignancies.

CBP-1018 is a PDC (peptide-drug conjugate) formed by conjugating Monomethyl auristatin E (HY-15162) to a dual-targeting ligand of FLOR1/PSMA (prostate-specific membrane antigen) via a linker (HY-78738). CBP-1018 binds to FLOR1 and prostate-specific membrane antigen (PSMA). CBP-1018 is applicable to the research of solid tumors and metastatic castration-resistant prostate cancer.

Cy5-ZW2-617 is a PSMA ligand with a IC₅₀ of 4.39 nM. Cy5-ZW2-617 specifically binds to PSMA and is thereby internalized by PSMA-positive cells. Cy5-ZW2-617 shows uptake in PSMA-positive tumor cells and tumor xenografts in mice. Cy5-ZW2-617 can be used for the research of prostate cancer.

PSMA ligand 1 (Compound 1c) is a PSMA ligand with an IC₅₀ of 26.74 nM. The [¹⁸F]-labeled PSMA ligand 1 can serve as a PSMA PET tracer and is used in research on the diagnosis of prostate cancer.

PSMA-SulfoCy7 is a high-affinity imaging agent targeting PSMA/GCPII (with a K_i of 18.1 nM for human PSMA). PSMA-SulfoCy7 regulates PSMA-dependent NAAG hydrolysis. PSMA-SulfoCy7 exhibits excellent in vivo imaging capability, enabling clear visualization of PSMA-expressing tumors in xenograft models, with no obvious toxicity even at a dose of 87.9 mg/kg. PSMA-SulfoCy7 is widely used in prostate cancer-related studies.

PSMA-1-SMCC is a selective binding agent targeting Prostate-Specific Membrane Antigen (PSMA). PSMA-1-SMCC is promising for research of targeted imaging for prostate cancer.

PSMA ligand 3 is a PSMA-targeting ligand of Psa-AR (HY-179056). Psa-AR can be used for cancer research.

PSMA ligand 2 is a prostate specific membrane antigen (PSMA) ligand with a glutamate-urea-lysine (GUL) moiety. PSMA ligand 2 can be efficiently labeled with radioactive nuclides such as ⁶⁸Ga and ¹⁷⁷Lu and specifically binds to PSMA-positive tumor cells. PSMA ligand 2 can be used for imaging of PSMA-expressing tumors or cells via PET or SPECT imaging. PSMA ligand 2 can be used for the research of prostate cancer.

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.

PSMA-trillium (Felivotide mopaxetan) is a PSMA-targeted molecule that contains a highly specific PSMA-binding motif, an albumin-binding domain optimized for tumor uptake and retention, and a Macropa chelator conjugated to the α-emitter ²²⁵Ac. PSMA-trillium binds to albumin to prolong plasma retention time and binds to PSMA via its specific motif. ²²⁵Ac-PSMA-Trillium exhibits dose-dependent inhibition of LNCaP tumor growth in mice. PSMA-trillium can be used in research related to prostate cancer and metastatic castration-resistant prostate cancer.

Ctx-L3 is a selective EGFR PTAC (PSMA-targeted chimera) degrader (DC₅₀: 4.3 pM in LNCaP cells) and LYTAC. Ctx-L3 recruits prostate-specific membrane antigen (PSMA) and mediates lysosomal degradation of EGFR in PSMA-positive prostate cancer cells. Ctx-L3 exhibits degrading activity against EGFR in prostate cancer cells. Ctx-L3 is applicable to related research on prostate cancer.

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.

PSMA-DIM is a dimeric PSMA ligand with a K_d of 37.09 nM for LNCaP cells. PSMA-DIM can be radiolabeled with [⁶⁸Ga]Ga to form [⁶⁸Ga]Ga-PSMA-DIM. [⁶⁸Ga]Ga-PSMA-DIM can effectively distinguish between cells and animal models with different expression levels of PSMA. [⁶⁸Ga]Ga-PSMA-DIM exhibits high LNCaP cells uptake and tumor uptake peak values. PSMA-DIM can be used for the study of prostate cancer (PCa).

NOTA-SP₂A-PSMAL is a ligand targeting prostate-specific membrane antigen (PSMA), which competitively binds to PSMA with high binding affinity and an IC₅₀ value of 0.26 nM. ¹⁸F-labeled NOTA-SP₂A-PSMAL can be used as a PET tracer for positron emission tomography imaging of prostate cancer. NOTA-SP₂A-PSMAL can be used for the synthesis and research of radionuclide conjugates (RDCs).

Atz-L5 is a PD-L1 PTAC (PSMA-targeted chimera) degrader (DC₅₀: 18 pM in PC3-PIP cells; 2 pM in LNCaP cells) and LYTAC. Atz-L5 promotes lysosomal degradation of PD-L1 in PSMA-positive prostate cancer cells. Atz-L5 is applicable to the research of prostate cancer.

PSMA-MAL-5 is a PSMA ligand. PSMA-MAL-5 covalently binds to Cys466 of PSMA. PSMA-MAL-5 labeled with ¹⁷⁷Lu and ²²⁵Ac has high radiostability and tumor uptake. PSMA-MAL-5 also effectively inhibits tumor growth. PSMA-MAL-5 can be used for SPECT/CT imaging and radionuclide therapy of prostate 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.