Home Others Drug-Linker Conjugates for ADC inhibitor Vipivotide tetraxetan (PSMA-617) For research use only.

Vipivotide tetraxetan (PSMA-617)

Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM.

Vipivotide tetraxetan (PSMA-617) Chemical Structure

Vipivotide tetraxetan (PSMA-617) Chemical Structure

CAS: 1702967-37-0

Selleck's Vipivotide tetraxetan (PSMA-617) has been cited by 1 publication

Purity & Quality Control

Batch: S867001 Water] 100 mg/mL] false] ] ] false] ] ] false Purity: 99.73%
99.73

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Biological Activity

Description Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM.
Targets
PSMA [1]
(Cell-free assay)
0.37 nM(Ki)
In vitro
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]
Cell Research Cell lines PSMA-positive LNCaP cell line
Concentrations 0–5000 nM
Incubation Time 1 h
Method

The cell-based assay is performed using 105 LNCaP cells/well. The radioligand (Glu-urea-Lys-(Ahx))2-[68Ga]Ga(HBED-CC)(19) is added as 0.75 nM solution to 12 different concentrations of non-labeled, natGa- or natLu-labeled PSMA-617 (from 0 to 5000 nM). After 1 hour incubation at 37 ℃, the cells are washed with ice-cold PBS and the cell-bound radioactivity is measured in a gamma counter.
In Vivo
In vivo

The 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.[1]
Animal Research Animal Models 8-wk-old BALB/c nu/nu mice which are subcutaneously inoculated into the right trunk with 5 × 106 LNCaP cells in 50% Matrigel.
Dosages ~30 MBq, 0.5 nM for small-animal PET imaging; ~1 MBq, 0.06 nM for organ distribution.
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05766371 Recruiting Castrate Resistant Prostate Cancer|Metastatic Castration-resistant Prostate Cancer|Prostate Cancer|Prostate Carcinoma University of California San Francisco|Merck Sharp & Dohme LLC|Prostate Cancer Foundation December 15 2023 Phase 2
NCT06004661 Not yet recruiting Metastatic Castration-Resistant Prostate Cancer (mCRPC) Novartis Pharmaceuticals|Novartis December 29 2023 Phase 2
NCT05228106 Recruiting Solid Cancers Centre de recherche du Centre hospitalier universitaire de Sherbrooke January 21 2022 --
NCT05219500 Recruiting Metastatic Castration Resistant Prostate Cancer Excel Diagnostics and Nuclear Oncology Center December 16 2021 Phase 2

Chemical lnformation & Solubility

Molecular Weight 1042.14 Formula

C49H71N9O16
CAS No. 1702967-37-0 SDF --
Smiles C1CC(CCC1CNC(=O)CN2CCN(CCN(CCN(CC2)CC(=O)O)CC(=O)O)CC(=O)O)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NCCCCC(C(=O)O)NC(=O)NC(CCC(=O)O)C(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Water : 100 mg/mL


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In vivo
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