1. Immunology/Inflammation
  2. PSMA
  3. PDI2

PDI2 (PSMA-DOTA-PEI2) 是一种前列腺特异性膜抗原 (PSMA) 配体,可用作肿瘤滞留剂、肾脏摄取降低剂、显像剂及抗肿瘤剂,用于 SPECT 诊断显像与放射诊疗。PDI2 特异性结合前列腺癌细胞上的 PSMA,通过网格蛋白依赖的内吞作用进入细胞,具有更高的肿瘤滞留率和更低的肾脏摄取水平。PDI2 可用于前列腺癌及去势抵抗性转移性前列腺癌的相关研究。

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PDI2

PDI2 Chemical Structure

CAS No. : 3110124-60-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that acts as a tumor retention agent, renal uptake reducer, imaging agent and antitumor agent, applicable in SPECT diagnostic imaging and radiotheranostics. PDI2 specifically binds to PSMA on prostate cancer cells, enters cells via clathrin-dependent endocytosis, and exhibits higher tumor retention rate and lower renal uptake level. PDI2 is applicable in research related to prostate cancer and castration-resistant metastatic prostate cancer[1].

体外研究
(In Vitro)

[111In]In-PDI2 (0.195-50 nM;冰上孵育 2 h) 可与 LNCaP 细胞上的 PSMA 特异性结合,Kd 值为 22.8 nM[1]
[111In]In-PDI2 (37 kBq;冰上结合 2 h,37℃ 孵育 0-4 h) 在 LNCaP 细胞的内化率为 38.9%[1]

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

体内研究
(In Vivo)

PDI2 (111 kBq; i.v.; 单剂量) 在 PSMA 阳性LNCaP前列腺癌异种移植模型中表现出较高且持续的肿瘤摄取,同时具有理想的肿瘤与肾脏放射性比值[1]
PDI2 (5-10 kBq; i.v.; 单剂量) 有效抑制 PSMA 阳性 LNCaP 前列腺癌异种移植物的生长,且无明显毒性[1]

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

Animal Model: BALB/c nu/nu (male, 5-6 weeks old)[1]
Dosage: 111 kBq
Administration: i.v.; single dose
Result: Measured 20.74% ID/g tumor accumulation at 4-h postinjection; measured 25.47% ID/g tumor accumulation at 24-h postinjection; measured 13.54% ID/g tumor accumulation at 96-h postinjection; measured 52.31% ID/g renal uptake at 4-h postinjection; measured 4.85% ID/g renal uptake at 24-h postinjection; achieved 7.3 tumor-to-kidney radioactivity ratio.
分子量

1271.41

Formula

C59H90N12O19

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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  • 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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产品名称:
PDI2
目录号:
HY-P11591
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