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前列腺癌是一種發生在前列腺中的癌癥,近年來隨著研究的進展,前列腺特異性膜抗原(PSMA)由于在大多數前列腺癌病灶中高表達而成為前列腺癌診斷和治療的新型標志物,這使其成為一種有前途的診斷靶點(通過正電子發射斷層掃描[PET]掃描成像)和放射配體療法的治療靶點。
1 、NOTA-PSMA
名稱 NOTA-PSMA
純度 98%
序列(單字母縮寫)
序列(三字母縮寫)
基本描述
分子量 941.05
化學式 C45H64N8O14
存儲條件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
編碼 04010027777
CAS
REFERENCES
分子圖
2 、PSMA
名稱 PSMA
純度 98%
序列(單字母縮寫) E-urea-K
序列(三字母縮寫) Glu-rea-Lys
基本描述
分子量 319.31
化學式 C12H21N3O7
存儲條件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
編碼 04010059069
CAS 1025796-69-3
REFERENCES
分子圖
3 、PSMA-617 Linker
名稱 PSMA-617 Linker
純度 95%
序列(單字母縮寫)
序列(三字母縮寫)
基本描述 Vipivotide tetraxetan Linker (PSMA-617 Linker) 是一種有效的不可降解的肽類 Linker,可用于合成 Vipivotide tetraxetan (PSMA-617)。Vipivotide tetraxetan (PSMA-617) 是用于合成?177Lu-PSMA-617 的配體,177Lu-PSMA-617 是用于研究前列腺癌的一種放射性分子。
分子量 655.74
化學式 C33H45N5O9
存儲條件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
編碼
CAS 1703768-74-4
REFERENCES Bene?ová M, et al. Albumin-Binding PSMA Ligands: Optimization of the Tissue Distribution Profile. Mol Pharm. 2018 Mar 5;15(3):934-946.
分子圖
4 、PSMA-617
名稱 PSMA-617
純度 98%
序列(單字母縮寫)
序列(三字母縮寫)
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
化學式 C49H71N9O16
存儲條件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
編碼 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
分子圖
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