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AMBA

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Catalog No. TP4415 Copy Product Info
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AMBA, a ligand for gastrin-releasing peptide receptor (GRPR, BB2, BRS-2), exhibits an IC50 of 0.82 nM and a Ki of 0.65 nM in human cells. It binds to GRPR with high specificity and affinity, leading to receptor-mediated endocytosis that retains conjugated radioactive metals within target cells. AMBA is applicable in prostate cancer research.

AMBA

Cas No. 721937-56-0
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
AMBA, a ligand for gastrin-releasing peptide receptor (GRPR, BB2, BRS-2), exhibits an IC50 of 0.82 nM and a Ki of 0.65 nM in human cells. It binds to GRPR with high specificity and affinity, leading to receptor-mediated endocytosis that retains conjugated radioactive metals within target cells. AMBA is applicable in prostate cancer research.
In vitro
AMBA exhibits high specificity and nanomolar affinity for the human GRPR receptor, with an IC50 of 0.82 nmol/L and a Ki of 0.65 nmol/L, within the concentration range of 0.001-1000 nmol/L over 60 minutes. Additionally, AMBA (6.66 × 10^-4 μmol (1 μg); 10 min) can be efficiently radiolabeled with 111 In, achieving a labeling efficiency of 95.43% under test conditions.
In vivo
Administered via a single intravenous injection, 111 In-AMBA (0.37 MBq-12.2 MBq/4 μg) reached a peak tumor uptake of 3.87% ID/g 8 hours post-injection in SCID mice bearing PC-3 prostate tumors. The maximum tumor-to-muscle ratio achieved was 11.79, indicating effective targeting of GRPR-expressing tumors.
Chemical Properties
Molecular Weight1502.70
FormulaC68H99N19O18S
Cas No.721937-56-0
SmilesC([C@H](NC([C@@H](NC(=O)C1=CC=C(NC(CNC(CN2CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC2)=O)=O)C=C1)CCC(N)=O)=O)C(N[C@H](C(N[C@H](C(NCC(N[C@@H](CC3=CN=CN3)C(N[C@H](C(N[C@@H](CCSC)C(N)=O)=O)CC(C)C)=O)=O)=O)[C@H](C)C)=O)C)=O)C=4C=5C(NC4)=CC=CC5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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:
mg/kg
g
µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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
Related Tags: AMBA in vivo | AMBA in vitro | AMBA formula | AMBA molecular weight