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前列腺癌是一种发生在前列腺中的癌症,近年来随着研究的进展,前列腺特异性膜抗原(PSMA)由于在大多数前列腺癌病灶中高表达而成为前列腺癌诊断和治疗的新型标志物,这使其成为一种有前途的诊断靶点(通过正电子发射断层扫描[PET]扫描成像)和放射配体疗法的治疗靶点。
1 、NOTA-PSMA
名称 NOTA-PSMA
纯度 98%
序列(单字母缩写)
序列(三字母缩写)
基本描述
分子量 941.05
化学式 C45H64N8O14
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
编码 04010027777
CAS
REFERENCES
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2 、PSMA
名称 PSMA
纯度 98%
序列(单字母缩写) E-urea-K
序列(三字母缩写) Glu-rea-Lys
基本描述
分子量 319.31
化学式 C12H21N3O7
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
编码 04010059069
CAS 1025796-69-3
REFERENCES
分子图
3 、PSMA-617 Linker
名称 PSMA-617 Linker
纯度 95%
序列(单字母缩写)
序列(三字母缩写)
基本描述 Vipivotide tetraxetan Linker (PSMA-617 Linker) 是一种有效的不可降解的肽类 Linker,可用于合成 Vipivotide tetraxetan (PSMA-617)。Vipivotide tetraxetan (PSMA-617) 是用于合成 177Lu-PSMA-617 的配体,177Lu-PSMA-617 是用于研究前列腺癌的一种放射性分子。
分子量 655.74
化学式 C33H45N5O9
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
编码
CAS 1703768-74-4
REFERENCES Benešová M, et al. Albumin-Binding PSMA Ligands: Optimization of the Tissue Distribution Profile. Mol Pharm. 2018 Mar 5;15(3):934-946.
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4 、PSMA-617
名称 PSMA-617
纯度 98%
序列(单字母缩写)
序列(三字母缩写)
基本描述 PSMA-617 is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM.
分子量 1042.14
化学式 C49H71N9O16
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
编码 04010047319
CAS 1702967-37-0
IN VITRO PSMA-617 demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated[1].
IN VIVO Organ distribution with 68Ga-labeled PSMA-617 after 1 h (n=3) reveals a high specific uptake in LNCaP tumors and in the kidneys. The high uptake in the kidneys is nearly completely blocked by coinjection of 2 mg o with the exception of the spleen. Tumor-to-background ratios are 7.8 (tumor to blood) and 17.1 (tumor to muscle) at 1 h after injection. As compared with the 68Ga-labeled version, the organ istribution with 177Lu-labeled PSMA-617 (n=3) show a similar uptake in the LNCaP tumors and in the kidneys. The liver uptake is found to be statistically different. Tumor-to-background ratios determined 1 h after injection show slightly higher values (tumor to blood, 22.1;tumor to muscle, 25.6) than previous organ distribution with 68Ga-labeled PSMA-617[1].
REFERENCES 1702967-37-0
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