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PSMA-IN-2

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Catalog No. T87271Cas No. 2946600-14-0

PSMA-IN-2, an inhibitor of PSMA with a K i value of 1.07 nM, exhibits favorable in vivo NIR imaging (λ EM = 1088 nm, λ ex = 808 nm) and is useful for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice [1].

PSMA-IN-2

PSMA-IN-2

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Catalog No. T87271Cas No. 2946600-14-0
PSMA-IN-2, an inhibitor of PSMA with a K i value of 1.07 nM, exhibits favorable in vivo NIR imaging (λ EM = 1088 nm, λ ex = 808 nm) and is useful for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice [1].
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
PSMA-IN-2, an inhibitor of PSMA with a K i value of 1.07 nM, exhibits favorable in vivo NIR imaging (λ EM = 1088 nm, λ ex = 808 nm) and is useful for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice [1].
Targets&IC50
PSMA:1.07 nM (Ki)
In vivo
PSMA-IN-2 (compound 24) (0.85 mg/kg, i.v., 24 h) is confirmed by NIR-II imaging to bind specifically to PSMA in vivo [1]. In 22Rv1 xenograft models [1], following an intravenous injection at a dosage of 0.85 mg/kg, the compound was excreted from the blood pool, leading to increased signal intensity in 22Rv1 xenografts over time as the background signal weakened under 808 nm laser irradiation (1100 nm long-pass filter, 400 ms), with inhibition ranging from 38% to 52% based on semi-quantitative data DCFPyL in tumors.
Chemical Properties
Molecular Weight1257.27
FormulaC54H60N14O18S2
Cas No.2946600-14-0
SmilesN(CCC(NCCCC[C@H](NC(N[C@@H](CNC=1C(=O)C(=O)C1O)C(O)=O)=O)C(O)=O)=O)(C)C2=CC=C(C=3C=4C(C(=C5C3N=S=N5)C6=CC=C(N(CCC(NCCCC[C@H](NC(N[C@@H](CNC=7C(=O)C(=O)C7O)C(O)=O)=O)C(O)=O)=O)C)C=C6)=NSN4)C=C2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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