psma-in-1

PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. It inhibits tumor growth with high selectivity and specificity in PSMA+ tumor models. Additionally, PSMA-IN-1 serves as an NIR (λEX: 620 nm; λEM: 670 nm) dye for tumor imaging. PSMA-IN-1 is utilized in prostate cancer research.

DL-Mannitol is a osmotic diuretic, it may play a role in reducing off-target 68Ga-PSMA renal uptake

Vipivotide tetraxetan linker is formed by conjugating the pharmacophore glutamic acid-urea-lysine peptide with a linker, and is mainly used in the synthesis of vipivotide tetraxetan (PSMA-617). The glutamic acid-urea-lysine motif specifically binds to prostate-specific membrane antigen (PSMA).

CQ-16 is an orally active small molecule drug conjugate (SMDC) that targets prostate-specific membrane antigen (PSMA). It exhibits high selectivity in its antiproliferative activity between PSMA-positive and PSMA-negative prostate cells. Additionally, CQ-16 possesses PARP inhibitory activity (IC50=1 nM).

GCPII-IN-1 is a potent inhibitor scaffold targeting glutamate carboxypeptidase II (GCPII), also known as prostate-specific membrane antigen (PSMA). It exhibits a high affinity for GCPII, with a binding affinity (K i ) of 44.3 nanomolar (nM).

GCPII-IN-1 TFA is a scaffold inhibitor of glutamate carboxypeptidase II (GCPII; PSMA) with a Ki of 44.3 nM.

Voxalatamab (JNJ-63898081), an IgG4 bispecific antibody targeting PSMA and CD3, demonstrates anti-cancer efficacy in prostate cancer research [1].

Pasotuxizumab (BAY 2010112) is a bispecific T-cell engager (BiTE) targeting PSMA and CD3, with dissociation constants (K D) of 47.0 nM for PSMA and 9.4 nM for CD3. It is used in the study of metastatic castration-resistant prostate cancer (mCRPC) [1] [2].

PSMA-IN-3 (compound 17) is a novel, high-affinity inhibitor of Prostate-Specific Membrane Antigen (PSMA) with an IC50 of 13 nM, showing potential for development as an 18F-labeled radioligand for PET imaging of PSMA in prostate cancer [1].

Lys(CO-C3-p-I-Ph)-O-tBu, a pharmacokinetic modifier (PK modifier), enhances the pharmacokinetic properties of PSMA ligand molecules by increasing their residence time in plasma through improved binding to albumin and reducing absorption by the salivary glands, potentially extending the active compound's half-life. Moreover, Ac-PSMA-trillium is an effective PSMA-targeting compound for various biological applications when modified with different radioactive isotopes. When labeled with 111 In, it serves as a DOTA chelating agent and imaging agent. Alternatively, when labeled with 225 Ac, it acts as a Macropa chelator for targeted radionuclide therapy (TRT) in researching metastatic castration-resistant prostate cancer (mCRPC) [1] [2].

PSMA-IN-2, an inhibitor of PSMA with a K i value of 1.07 nM, exhibits favorable in vivo NIR imaging (λ EM = 1088 nm, λ ex = 808 nm) and is useful for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice [1].

PSMA-IN-4 (compound 9) functions as a potent PSMA inhibitor, exhibiting an IC 50 value of 1.2 μM [1].

PSMA-Val-Cit-PAB-Azide, a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), incorporates a cleavable linker (Val-Cit-PAB) and a novel small-molecule conjugate targeting PSMA. This compound features an Azide group, enabling it to participate in the copper-catalyzed azide-alkyne cycloaddition reaction (CuAAC) with Alkyne-group-containing molecules [1].

DL-Mannitol (Standard) is the standard substance of DL-Mannitol, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. DL-Mannitol is a osmotic diuretic, it may play a role in reducing off-target 68Ga-PSMA renal uptake

PSMA-1-SMCC is a selective ligand that targets the prostate-specific membrane antigen (PSMA). It holds potential for research applications in the targeted imaging of prostate cancer.

JR11-PEG3-HBED-CC-PSMA-03 (Compound 1) is an RDC-related compound comprising the chelator HBED-CC, the JR11 peptide (an SSTR2 antagonist), and a PSMA ligand. It binds to SSTR2 and PSMA with IC50 values of 59.2 nM and 57.0 nM, respectively. This compound can be radiolabeled with [68Ga], and the [68Ga]-labeled JR11-PEG3-HBED-CC-PSMA-03 is utilized in diagnostic research for neuroendocrine-differentiated prostate cancer.