Vipivotide tetraxetan (PSMA-617)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
100mg	$3750	To Be Confirmed
200mg	$5625	To Be Confirmed
500mg	$9450	To Be Confirmed

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Cat #: V5114 CAS #: 1702967-37-0 Purity ≥ 98%

Description: Vipivotide tetraxetan (also known as PSMA-617) is a novel and highly potent prostate-specific membrane antigen (PSMA) inhibitor with anticancer activity. It inhibits PSMA with a Ki of 0.37 nM. Vipivotide tetraxetan is a ligand used to make 177Lu-PSMA-617 [Pluvicto (lutetium (177Lu) vipivotide tetraxetan)], which is a radioactive molecule approved in 2022 to combat cancer. PSMA-617 originally was developed at the German Cancer Research Center and the Heidelberg University Hospital. ABX held the exclusive license to bring the treatment through early clinical development.

References: [1]. Benešová M, et al. Preclinical Evaluation of a Tailor-Made DOTA-Conjugated PSMA Inhibitor with Optimized Linker Moiety for Imaging and Endoradiotherapy of Prostate Cancer. J Nucl Med. 2015 Jun;56(6):914-20.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	1042.14
Molecular Formula	C₄₉H₇₁N₉O₁₆
CAS No.	1702967-37-0
Storage	-20℃ for 3 years in powder formrrr
Storage	-80℃ for 2 years in solvent
SMILES Code	O=C(O)CC[C@@H](C(O)=O)NC(N[C@@H](CCCCNC([C@H](CC1=CC=C2C=CC=CC2=C1)NC([C@H]3CC[C@H](CNC(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)=O)=O)C(O)=O)=O
Synonyms	WHO-11010; WHO11010; WHO 11010; Vipivotide tetraxetan; PSMA-617; PSMA617; PSMA 617;

Protocol	In Vitro	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.
Protocol	In Vivo	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).

These protocols are for reference only. InvivoChem does not independently validate these methods.

Related Biological Data

Time–activity-curves for tumor and background (A) and for relevant organs (B) up to 1 h after injection of 0.5 nmol of 68Ga-labeled PSMA-617. Data are mean standardized uptake value (SUVmean).

Whole-body coronal slices from small-animal PET imaging of athymic male nude mouse bearing LNCaP tumor xenografts. Tumor-targeting efficacy and pharmacokinetic properties were evaluated by injection of 0.5 nmol of 68Ga-labeled PSMA-617 (∼30 MBq) with following scans at 0–20 min (A), 20–40 min (B), 40–60 min (C), and 120 min (D) after injection.

Whole-body coronal scans as maximum-intensity projections at 60 (A) and 120 min (B) after injection of 68Ga-labeled PSMA-617.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	0.9596 mL	4.7978 mL	9.5956 mL	19.1913 mL
5mM	0.1919 mL	0.9596 mL	1.9191 mL	3.8383 mL
10mM	0.0960 mL	0.4798 mL	0.9596 mL	1.9191 mL
20mM	0.0480 mL	0.2399 mL	0.4798 mL	0.9596 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.