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 No. 1702967-37-0

Purity & Quality Control

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

Vipivotide tetraxetan (PSMA-617) Related Products

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
NCT06303713 Not yet recruiting
Prostate Cancer|Metastatic Prostate Cancer|Metastatic Castration-resistant Prostate Cancer
Dana-Farber Cancer Institute|Novartis
 May 2024 Phase 1
NCT06004661 Recruiting
Metastatic Castration-Resistant Prostate Cancer (mCRPC)
Novartis Pharmaceuticals|Novartis
 April 4 2024 Phase 2
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
NCT05228106 Recruiting
Solid Cancers
Centre de recherche du Centre hospitalier universitaire de Sherbrooke
 January 21 2022 --

Chemical Information & 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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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