Vipivotide tetraxetan (Synonyms: PSMA-617)

Name: Vipivotide tetraxetan
Brand: MedChemExpress
SKU: HY-117410
Rating: 5.0 (9 reviews)

Cat. No.: HY-117410 Purity: 99.57%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a K_i of 0.37 nM. Vipivotide tetraxetan (PSMA-617) is designed consisting of three components: the pharmacophore Glutamate-urea-Lysine, the chelator DOTA able to complex both 68Ga or 177Lu, and a linker connecting these two entities. Glutamate-urea-Lysine is the selective pharmacophore to bind to prostate specific membrane antigen.

For research use only. We do not sell to patients.

Vipivotide tetraxetan Chemical Structure

CAS No. : 1702967-37-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 1433	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 1433	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 770	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2990	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE Vipivotide tetraxetan

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

Traditional Cytotoxic Agents

In Vitro

Vipivotide tetraxetan (PSMA-617) demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant K_i=2.34±2.94 nM on LNCaP; K_i=0.37±0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

1042.14

Formula

C₄₉H₇₁N₉O₁₆

CAS No.

1702967-37-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[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)NC(N[C@H](C(O)=O)CCC(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (119.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 100 mg/mL (95.96 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.9596 mL	4.7978 mL	9.5956 mL
5 mM	0.1919 mL	0.9596 mL	1.9191 mL
10 mM	0.0960 mL	0.4798 mL	0.9596 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.57%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (246 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	0.9596 mL	4.7978 mL	9.5956 mL	23.9891 mL
	5 mM	0.1919 mL	0.9596 mL	1.9191 mL	4.7978 mL
	10 mM	0.0960 mL	0.4798 mL	0.9596 mL	2.3989 mL
	15 mM	0.0640 mL	0.3199 mL	0.6397 mL	1.5993 mL
	20 mM	0.0480 mL	0.2399 mL	0.4798 mL	1.1995 mL
	25 mM	0.0384 mL	0.1919 mL	0.3838 mL	0.9596 mL
	30 mM	0.0320 mL	0.1599 mL	0.3199 mL	0.7996 mL
	40 mM	0.0240 mL	0.1199 mL	0.2399 mL	0.5997 mL
	50 mM	0.0192 mL	0.0960 mL	0.1919 mL	0.4798 mL
	60 mM	0.0160 mL	0.0800 mL	0.1599 mL	0.3998 mL
	80 mM	0.0120 mL	0.0600 mL	0.1199 mL	0.2999 mL
DMSO	100 mM	0.0096 mL	0.0480 mL	0.0960 mL	0.2399 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Vipivotide tetraxetan Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vipivotide tetraxetan1702967-37-0PSMA-617PSMA617PSMA 617Drug-Linker Conjugates for ADCInhibitorinhibitorinhibit

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Vipivotide tetraxetan (Synonyms: PSMA-617)

Customer Review

Vipivotide tetraxetan Related Antibodies

9 Publications Citing Use of MCE Vipivotide tetraxetan

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Drug-Linker Conjugates for ADC Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Vipivotide tetraxetan Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Vipivotide tetraxetan Related Classifications

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