|
名稱 |
PSMA-617 |
|
純度 |
98% |
|
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]. |
