2. 疾病领域
  3. 癌症 泌尿生殖系统疾病
  4. 前列腺癌 泌尿生殖系统癌症
  5. PSMA-1-DOTA

PSMA-1-DOTA 是一种高亲和力的前列腺特异性膜抗原 (PSMA) 结合剂，可实现用于成像与治疗的靶向放射性核素递送。PSMA-1-DOTA 可作为肿瘤生长抑制剂，能够抑制表达 PSMA 的前列腺肿瘤的生长。

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PSMA-1-DOTA

PSMA-1-DOTA Chemical Structure

CAS No. : 3024672-17-8

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PSMA-1-DOTA 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PSMA-1-DOTA is a prostate-specific membrane antigen (PSMA) binder with high affinity, enables targeted radionuclide delivery for imaging and therapy. PSMA-1-DOTA acts as a tumor growth inhibitor that reduces growth of PSMA-expressing prostate cancer tumors[1].

体外研究
(In Vitro)

PSMA-1-DOTA (1 h) 可抑制 ³H-ZJ24 与 PC3pip 细胞的结合，其 IC50 为 1.83 nM，对 PSMA 的亲和力约为 PSMA-I&T 和 PSMA-11 的 4 倍[1]。

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

PSMA-1-DOTA 相关抗体:
体内研究
(In Vivo)

PSMA-1-DOTA (1.4 mg/kg；i.v.；单剂量) 在NMRI小鼠中耐受性良好，仅在淋巴组织中出现轻微的组织病理学改变[1]。
[177Lu]Lu-PSMA-1-DOTA (总剂量 111 MBq，2 天内分 4 次给药，每次 27.75 MBq；或 111 MBq 单剂量；静脉注射) 可有效抑制 PC3pip 异种移植小鼠的肿瘤生长达 24 天[1]。
[68Ga]Ga-PSMA-1-DOTA (7.4 MBq；静脉注射) 在异种移植小鼠体内可靶向 PC3pip 肿瘤，同时在肾脏和唾液腺中的非靶标摄取量极低[1]。

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

Animal Model: athymic nude [Foxn1/nu/Foxn1/nu] (male, 6-8 weeks old, PC3pip subcutaneous xenograft model)[1]
Dosage: 111 MBq (3 mCi) total, 4 doses of 27.75 MBq each over 2 days; 111 MBq (3 mCi) single dose
Administration: i.v.; 4 doses over 2 days (day 0); single dose (day 13)
Result: Eliminated tumor growth for 24 days; achieved tumor inhibitory activity comparable to [¹⁷⁷Lu]Lu-PSMA-617 (positive control).
Animal Model: athymic nude [Foxn1/nu/Foxn1/nu] (male, PC3pip subcutaneous xenograft model)[1]
Dosage: 7.4 MBq (200 μCi)
Administration: i.v.
Result: Showed significantly lower kidney and salivary gland uptake compared to [⁶⁸Ga]Ga-PSMA-11 and [⁶⁸Ga]Ga-PSMA I&T; reached tumor-to-left salivary gland ratio of 13.45 at 30 minutes and 27.43 at 1 hour post-injection.
Animal Model: NMRI (male, 8 weeks old)[1]
Dosage: 1.4 mg/kg
Administration: i.v.; single dose
Result: Observed no mortality, significant body weight changes, or abnormal clinical signs; detected no significant changes in clinical chemistry parameters on day 2 or day 15; identified test item-related histopathological changes in spleen, bone marrow, and inguinal lymph nodes (present after 14-day recovery).
分子量

1473.54

Formula

C62H100N14O27
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

PSMA-1-DOTA 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

PSMA-1-DOTA3024672-17-8metastatic castration-resistant prostate cancerprostate cancerlacrimal glandsPC3pip cellsprostate-specific membrane antigenPET imaging agentNMRI micekidneyssalivary glandsPC3pip xenograft miceInhibitorinhibitorinhibit

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