Vipivotide tetraxetan

Research use only, not for human use.

Vipivotide tetraxetan is a high potent inhibitor of prostate-specific membrane antigen (PSMA)(Ki of 0.37 nM).

Vipivotide tetraxetan is a high potent inhibitor of prostate-specific membrane antigen (PSMA)(Ki of 0.37 nM).(In Vitro):Vipivotide tetraxetan demonstrated high radihigh inhibition potency, highly efficient internalization into LNCaP cells and olytic stability for at least 72 h.(In Vivo):The small-animal PET measurements showed high tumor-to-background contrasts as early as 1 h after injection of Vipivotide tetraxetan. Organ distribution revealed specific uptake in LNCaP tumors and in the kidneys 1 h after injection of Vipivotide tetraxetan.

Vipivotide tetraxetan (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.

Organ distribution with 68Ga-labeled Vipivotide tetraxetan (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 Vipivotide tetraxetan (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 Vipivotide tetraxetan (PSMA-617).

PSMA-617

Others

Other Targets

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1702967-37-0

1042.154

C49H71N9O16

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (119.95 mM)

OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H]1CC[C@H](CNC(=O)CN2CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC2)CC1)C(O)=O)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years