Home Proteases PSMA inhibitor Vipivotide tetraxetan (PSMA-617)

research use only

Vipivotide tetraxetan (PSMA-617) PSMA inhibitor

Cat.No.S8670

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) PSMA inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 1042.14

Jump to

Quality Control

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

Solubility

In vitro
Batch:

Water : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 1042.14 Formula

C49H71N9O16

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1702967-37-0 -- Storage of Stock Solutions

Synonyms N/A 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

Mechanism of Action

Targets/IC50/Ki
PSMA
(Cell-free assay)
0.37 nM(Ki)
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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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 --

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.