Home Tools
Log in
Cart

AMG 487

Catalog No. T10297L   CAS 473719-41-4

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
AMG 487 Chemical Structure
AMG 487, CAS 473719-41-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 70.00
5 mg In stock $ 117.00
10 mg In stock $ 167.00
25 mg In stock $ 282.00
50 mg In stock $ 418.00
100 mg In stock $ 618.00
1 mL * 10 mM (in DMSO) In stock $ 156.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.88%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
Targets&IC50 [125I]-IP10-CXCR3:8 nM, [125I]-ITAC-CXCR3:8.2 nM
In vitro AMG487 is a small molecular weight antagonist of CXCR3. 66.1 tumor cells were pretreated with AMG487 prior to i.v. injection into immune-competent female mice. Antagonism of CXCR3 on 66.1 tumor cells inhibited experimental lung metastasis, and this antimetastatic activity was compromised in mice depleted of natural killer cells. Systemic administration of AMG487 also inhibited experimental lung metastasis. In contrast to the antimetastatic effect of AMG487, local growth of 66.1 mammary tumors was not affected by receptor antagonism. Murine mammary tumor cells express CXCR3 which facilitates the development of lung metastases.Indicate for the first time that a small molecular weight antagonist of CXCR3 has the potential to inhibit tumor metastasis[2].
In vivo AMG487, a small molecular weight antagonist. In vivo, systemic CXCR3 antagonism by preventive or curative treatments with AMG487 markedly inhibited the implantation and the growth of human and mouse CRC cells within lung without affecting that in the liver. In addition, we measured increased levels of CXCR3 and ligands expression within lung nodules compared with liver tumours. Activation of CXCR3 receptors by its cognate ligands facilitates the implantation and the progression of CRC cells within lung tissues and that inhibition of this axis decreases pulmonary metastasis of CRC in two murine tumour models[3].
Molecular Weight 603.59
Formula C32H28F3N5O4
CAS No. 473719-41-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41 mg/mL (67.93 mM)

TargetMolReferences and Literature

1. Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. 2. Walser TC, et al. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 2006 Aug 1;66(15):7701-7. 3. Cambien B, et al. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br J Cancer. 2009 Jun 2;100(11):1755-64. 4. Henne KR, et al. Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. Drug Metab Dispos. 2012 Jul;40(7):142

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Immuno-Oncology Compound Library NO PAINS Compound Library Bioactive Compound Library Orally Active Compound Library Inhibitor Library Autophagy Compound Library Immunology/Inflammation Compound Library Chemokine Inhibitor Library Cytokine Inhibitor Library

Related Products

Related compounds with same targets
Motixafortide TFA(664334-36-5,Free) Mogamulizumab Ulocuplumab Burixafor hydrobromide MSX-122 DOTA-CXCR4-L NUCC-390 dihydrochloride (1060524-97-1 free base) SDF-1α (human)

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

AMG 487 473719-41-4 Autophagy GPCR/G Protein Immunology/Inflammation CXCR Metastatic metastasis inhibit cancer CXCL11 CXC chemokine receptors CXCL10 chemokine AMG487 AMG-487 receptor CXCR3 Inhibitor Breast colon inhibitor

 

TargetMol