Zopocianine  (Synonyms: OTL-0078; OTL78)

Zopocianine (OTL-0078; OTL78) is a near-infrared optical probe targeting PSMA. Zopocianine binds to PSMA on the surface of PSMA-expressing cells, enters cells via receptor-mediated endocytosis, and accumulates in acidic endosomes. Zopocianine selectively accumulates in PSMA-positive cancer tissues and enables the detection of small tumors, primary prostate tumors, and locoregional metastases. Zopocianine helps achieve negative tumor surgical margins during fluorescence-guided surgery. Zopocianine is applicable to research related to prostate cancer^[1].

Zopocianine (0.001 nmol/L-10 μmol/L; 30 min at 4°C) competes for PSMA binding on 22Rv1 human prostate cancer cells with an IC₅₀ of 7 nmol/L^[1].
Zopocianine (0-120 nmol/L; 30 min at 4°C) binds directly to PSMA⁺ 22Rv1 human prostate cancer cells with a K_d of 4.7 nmol/L, and shows no significant binding to PSMA^- PC3 human prostate cancer cells^[1].
Zopocianine (100 nmol/L; 1 h at 37°C, 1 h at 4°C) binds to the cell surface of PSMA⁺ 22Rv1 and LNCaP human prostate cancer cells at 4°C, and undergoes PSMA-mediated internalization into acidic endosomes at 37°C, with no detectable binding to PSMA^- PC3 human prostate cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Zopocianine (0.3-120 nM/mouse; intravenous injection; single administration) selectively accumulates in PSMA-expressing subcutaneous prostate cancer xenografts in nude mice and orthotopic prostate cancer xenografts in SCID mice, enabling fluorescence-guided surgery and achieving negative surgical margins in nude mice bearing subcutaneously inoculated prostate cancer xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1640.82

C₇₄H₉₃N₇O₂₇S₄

2206660-94-6

Solid

Green to dark green

O=S(CCCCN1C2=CC=C(S(=O)(O)=O)C=C2C(C)(/C1=C/C=C3C(OC4=CC=C(C=C4)C[C@@H](C(O)=O)NC([C@@H](NC(CCOCCOCCNC(CC[C@@H](C(O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O)=O)=O)CC5=CC=CC=C5)=O)=C(CCC/3)/C=C\C6=[N+](C7=CC=C(S(=O)(O)=O)C=C7C6(C)C)CCCCS(=O)([O-])=O)C)(O)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Kularatne SA, et al. Evaluation of Novel Prostate-Specific Membrane Antigen-Targeted Near-Infrared Imaging Agent for Fluorescence-Guided Surgery of Prostate Cancer. Clin Cancer Res. 2019;25(1):177-187.  [Content Brief]