1702967-37-0
1702967-37-0 structure
- Name: PSMA-617
- Chemical Name: PSMA-617
- CAS Number: 1702967-37-0
- Molecular Formula: C49H71N9O16
- Molecular Weight: 1042.14
- Catalog: Research Areas Cancer
- Create Date: 2019-01-20 10:07:19
- Modify Date: 2024-01-02 19:09:27
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PSMA-617 is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM.
| Name | PSMA-617 |
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| Description | PSMA-617 is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM. |
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| Related Catalog | |
| Target |
Ki: 0.37 nM (PSMA)[1]. |
| 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 of 2-PMPA per kilogram. Other organs such as the liver, lung, and spleen show rather low uptake and no blocking effect, 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 distribution 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 |
| Molecular Formula | C49H71N9O16 |
|---|---|
| Molecular Weight | 1042.14 |