PSMA

Vipivotide tetraxetan (PSMA-617) is a highly potent inhibitor of prostate-specific membrane antigen (PSMA) with a Ki of 0.37 nM.

PSMA-11 (HBED-CC-PSMA) detects prostate cancer recurrence and metastasis by binding to the extracellular structural domain of prostate-specific membrane antigen (PSMA).PSMA-11 is often used as a tracer of PSMA-expressing tumours in positron emission tomography (PET) scanning by intravenous injection of gallium Ga 68-labelled PSMA-11, Glu-urea-Lys(Ahx) molecule targeted and bound PSMA-expressing tumour cells. After internalisation, PSMA-expressing tumour cells could be detected on PET imaging.

PSMA I&T is a PSMA-targeting radiocompound that serves as a diagnostic agent for prostate-specific membrane antigen-targeted therapy, often coupled with radioactivity.

Rosopatamab MMAE (HUJ-591 MMAE) is an ADC consisting of a PSMA-directed antibody (humanized IgG1 monoclonal antibody against PSMA and monomethylauristatin E (MMAE) for prostate cancer research.

HUHS015 is a potent PCA-1/ALKBH3 inhibitor.

Glu-urea-Lys is a molecular scaffold that targets PSMA and can be used as a prostate cancer imaging agent to study prostate-specific membrane antigens.

Piflufolastat (DCFPYL) is a PET imaging agent for prostate cancer PSMA. It is a fluorinated prostate-specific membrane antigen (PSMA) preparation. Piflufolastat can be used to prepare piflufolastat F 18 (DCFPyL F-18).

DUPA (N,N''-Carbonylbis[L-glutamic acid]) is used as the targeting moiety to actively deliver DTX for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.

Rosopatamab is a humanized monoclonal antibody targeting prostate-specific membrane antigen (PSMA) for the treatment of prostate cancer. It can be conjugated with radiolabeled isotopes (e.g., 177Lu) via DOTA-NHS ester to form radiopharmaceuticals for targeted therapy. In preclinical studies, 177Lu-DOTA-Rosopatamab combined with the DNA-PK inhibitor Peposertib achieved a 75% complete response rate in prostate cancer mouse models.

Isosilybin B is a flavonolignan extracted from silymarin that exhibits anti-prostate cancer (PCA) activity, inhibits cancer cell proliferation, and contributes to G1-phase blockade and apoptosis.Isosilybin B induces degradation of the androgen receptor.

CS-0047390, also known as tert-Butyl-DCL, PSMA inhibitor, is a radiopaque peptide reagent.

DUPA(OtBu)-OH is a precursor of DUPA, which is used as a targeting moiety to actively deliver Docetaxel (DTX) for treating Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer, with PSMA showing high affinity for DUPA (Ki = 8 nM).

Pelgifatamab (BAY-2315497) is a prostate-specific membrane antigen (PSMA) antibody with potential anticancer activity that can be used to study prostate cancer.

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

Biotin-NH-PSMA-617 is a biotinylated derivative of the small molecule PSMA-617, designed to target prostate-specific membrane antigen (PSMA), which is prominently expressed on prostate tumor cells. The biotinylation of PSMA-617 enhances its ability to bind PSMA, making it a valuable tool in the targeting of prostate cancer cells for diagnostic and therapeutic applications.

PSMA-ALB-56 is a PSMA-targeting radioactive ligand with antitumor activity, composed of glutamic urea PSMA binding entities, DOTA chelating agents, and albumin binders based on 4-(p-iodophenyl)- fragment or p(tolyl)- fragment.

Glu-urea-Lys TFA (1025796-69-3 free base) is a PSMA inhibitor.

BQ0413 exhibits high affinity for PSMA, with a dissociation constant (KD) of 89 pM. It demonstrates effective uptake and internalization, with an internalization rate of 44% in PC3-pip cells. After being labeled with [99mTc], BQ0413 can serve as an imaging agent for tumors.

Prostate Specific Antigen Substrate is a fluorescent substrate specific to prostate-specific antigen (PSA), facilitating the detection of PSA enzymatic activity [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.

Ac-macropa is a conjugate of Actinium-225 that targets PSMA, and it is useful for researching prostate cancer.

PSMA-trillium is a PSMA-targeting compound comprising a PSMA-targeting molecule (PSMA binding agent), a Macropa chelator, and a pharmacokinetics-modulating group (PK modulator). It acts as the non-radioactive variant of Actinium-225-PSMA-Trillium (BAY 3563254), boasting enhanced PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind with Ac through either the Macropa chelator or the radioactive isotope Actinium-225. Actinium-225-PSMA-Trillium effectively inhibits metastatic castration-resistant prostate cancer (mCRPC).

BQ7876 is a probe that targets prostate-specific membrane antigen (PSMA) and contains a DOTA chelator. After radiolabeling with radionuclides (177Lu), BQ7876 specifically binds to PSMA, serving both in radionuclide imaging and tumor cell destruction. It shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC). BQ7876 can also be utilized in the synthesis/research of radionuclide conjugated drugs (RDC).

Defactinib analogue-1 (Compound 7) serves as a ligand for the target protein FAK, and is utilized in the synthesis of PROTAC FAK degrader 1.