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

目录号: HY-159500A
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Zopocianine sodium (OTL-0078 sodium; OTL78 sodium) 是一种靶向 PSMA 的近红外光学探针。Zopocianine sodium 可与表达 PSMA 的细胞表面 PSMA 结合,经受体介导的内吞作用进入细胞,并滞留于酸性内体中。Zopocianine sodium 可选择性聚集于 PSMA 阳性癌组织,能够检测小型肿瘤、原发性前列腺肿瘤及局部区域转移灶。Zopocianine sodium 可在荧光引导手术中帮助实现肿瘤手术切缘阴性。Zopocianine sodium 可用于前列腺癌的相关研究。

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Zopocianine sodium

Zopocianine sodium Chemical Structure

CAS No. : 2206660-95-7

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  • 生物活性

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生物活性

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].

体外研究
(In Vitro)

Zopocianine (0.001 nM-10 μM; 30 min at 4°C) sodium 可在 22Rv1 人前列腺癌细胞上竞争性结合 PSMA,其 IC50 为 7 nM[1]
Zopocianine (0-120 nM; 30 min at 4°C) sodium 可直接与 PSMA+ 22Rv1 人前列腺癌细胞结合,其 Kd 值为 4.7 nM,且与 PSMA- PC3 人前列腺癌细胞无显著结合作用[1]
Zopocianine (100 nM; 1 h at 37°C, 1 h at 4°C) sodium 可在 4°C 下结合 PSMA+人前列腺癌细胞 22Rv1 和 LNCaP 的细胞表面,在 37°C 下经 PSMA 介导内吞进入酸性内体,且与 PSMA-人前列腺癌细胞 PC3 无可检测到的结合[1]

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

体内研究
(In Vivo)

Zopocianine (0.3-120 nM/mouse;静脉注射;单次) sodium 可在裸鼠的 PSMA 表达型皮下前列腺癌、SCID 小鼠的原位前列腺癌异种移植物中选择性聚集,实现荧光引导手术,使皮下接种前列腺癌异种移植物的裸鼠获得阴性手术切缘[1]

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

Animal Model: nu/nu (nude) (7-week-old, male; subcutaneous xenograft model with 22Rv1 cells)/SCID (7-week-old, male; orthotopic xenograft model with 22Rv1 cells)[1]
Dosage: 0.3 nM/mouse, 1 nM/mouse, 3 nM/mouse, 10 nM/mouse, 30 nM/mouse, 120 nM/mouse
Administration: i.v.; single bolus injection
Result: Provided an excellent tumor-to-background ratio (TBR) and accumulates within orthotopic prostate tumors.
Enabled fluorescence-guided surgery, achieving a 100% tumor-free survival rate at 30 days, with no observed biochemical recurrence.
Generated high-quality tumor images.
分子量

1662.80

Formula

C74H92N7NaO27S4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Zopocianine sodium
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HY-159500A
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