Vipivotide tetraxetan (PSMA-617) (C09-1082-693)

InformationVipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM.TargetsPSMA (Cell-free assay) 0.37 nM(Ki)In vitroPSMA-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.In vivoThe small-animal PET measurements show high tumor-to-background contrasts as early as 1 h after injection. In vivo distribution reveals specific uptake in LNCaP tumors and in the kidneys 1 h after injection. With regard to therapeutic use, PSMA-617 exhibits a rapid clearance from the kidneys from 113.3 ± 24.4 at 1 h to 2.13 ± 1.36 percentage injected dose per gram at 24 h. The favorable pharmacokinetics of the molecule leads to tumor-to-background ratios of 1,058 (tumor to blood) and 529 (tumor to muscle), respectively,24 h after injection.Cell Research(from reference)Cell lines：PSMA-positive LNCaP cell line Concentrations：0–5000 nM Incubation Time：1 h. Specifications and Purity: 98%. Molecular Formula: C49H71N9O16. Molecular Weight: 1042.14. PubChem CID: 122706786. Isomeric SMILES: C1CC(CCC1CNC(=O)CN2CCN(CCN(CCN(CC2)CC(=O)O)CC(=O)O)CC(=O)O)C(=O)N[C@@H](CC3=CC4=CC=CC=C4C=C3)C(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O. Related Document: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/V414106-SCI_addcd4d72e1e45d433426f11b50bb4b9.pdf.