Zopocianine sodium  (Synonyms: OTL-0078 sodium; OTL78 sodium)

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

Zopocianine (0.001 nM/L-10 μmol/L; 30 min at 4°C) sodium competes for PSMA binding on 22Rv1 human prostate cancer cells with an IC₅₀ of 7 nM/L^[1].
Zopocianine (0-120 nM/L; 30 min at 4°C) sodium 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 nM/L; 1 h at 37°C, 1 h at 4°C) sodium 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) sodium 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.

1662.80

C₇₄H₉₂N₇NaO₂₇S₄

2206660-95-7

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zopocianine (OTL-0078; OTL78). WHO Drug Information, Vol. 37, No. 4, 2023.