1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

AMG 487 (Synonyms: AMG487; AMG-487)

Cat. No.: HY-15319 Purity: 99.65% ee.: 99.97%
Data Sheet SDS Handling Instructions

AMG 487 is an antagonist of the chemokine receptor CXCR3, which inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 with IC50 values of 8.0 and 8.2 nM, respectively.

For research use only. We do not sell to patients.
AMG 487 Chemical Structure

AMG 487 Chemical Structure

CAS No. : 473719-41-4

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $159 In-stock
5 mg $120 In-stock
10 mg $170 In-stock
50 mg $640 In-stock
100 mg $980 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

AMG 487 is an antagonist of the chemokine receptor CXCR3, which inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 with IC50 values of 8.0 and 8.2 nM, respectively.

IC50 & Target

IC50: 8.0 nM (125I-IP-10 binding to CXCR3), 8.2 nM (125I-ITAC binding to CXCR3)

In Vitro

AMG 487 inhibits CXCR3-mediated cell migration by the three CXCR3 chemokines (IP-10 IC50=8 nM, ITAC IC50=15 nM, and MIG IC50=36 nM). Furthermore, AMG 487 inhibits calcium mobilization in response to ITAC (IC50=5 nM)[1]. AMG487 (1 μM) develops into fewer lung metastases, and the lungs are significantly smaller than vehicle-treated lungs[2]. AMG487 abrogates proliferation/survival of C26 tumour cells[3].

In Vivo

AMG 487 (0.03-10 mg/kg, s.c.) exhibits significant reduction in cellular infiltration into the lungs in a dose dependent manner[1]. AMG487 (5 mg/kg, s.c., twice daily) develops fewer metastases than that in vehicle-treated mice[2]. AMG487 (5 mg/kg, s.c.)-treated mice exhibits fewer pulmonary nodules than the control mice in both the models. AMG487 reduces the tumour volume[3].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.6568 mL 8.2838 mL 16.5675 mL
5 mM 0.3314 mL 1.6568 mL 3.3135 mL
10 mM 0.1657 mL 0.8284 mL 1.6568 mL
Kinase Assay
[3]

Cells are then lysed and sonicated in 50 mM Hepes pH 7.5, 150 mM NaCl, 20 mM EDTA, 1 mM PMSF, 10 μg/mL leupeptin, 2 μg/mL aprotinin and 0.2% NP-40. Equal amount of lysates are mixed in substrate buffer (50 mM Hepes, 100 mM NaCl, 1 mM EDTA, 10% sucrose, 0.5% CHAPS, 5 mM dithiothreitol) with Ac-DEVD-AMC substrate and caspase-3/7 substrate in a microtiter plate. Production of fluorigenic substrate is measured continuously at 37°C in a spectrophotometer Ascent Fluoroskan and the caspase activity (expressed as U/mg of protein) is defined as the amount of enzyme cleaving 1 nmol of substrate/min.

Cell Assay
[3]

AMG 487 is prepared as a 10 mM stock with DMSO. 

Colon cancer cells are seeded at a density of 104 cells cm2 and incubated either in serum-enriched medium or in base medium (containing 0.1% bovine serum albumin, BSA) supplemented or not with various concentrations of rCXCL9, rCXCL10 and rCXCL11 for the indicated periods of time before being either trypsin-detached, collected and enumerated or re-fed with fresh medium for 3 days, harvested and enumerated. The morphology of the CRC cells is observed through an inverted optical microscope at ×20 magnification, and photographs are taken at day 7.

Animal Administration
[2]

AMG487 is formulated in 20% of hydroxypropyl-β-cyclodextrin.

Local tumor growth and spontaneous metastasis are evaluated by injecting 3×105 viable tumor cells s.c. proximal to the right abdominal mammary gland of syngeneic female mice. Tumor diameters are measured by caliper twice weekly, and mice are euthanized on an individual basis when the s.c. tumor measured 18 mm in diameter or earlier if the mouse seemed moribund. The lungs are removed and weighed, and surface tumor colonies are quantified in a blinded fashion under a dissecting microscope. Experimental metastasis is evaluated by injecting 9×104 viable tumor cells i.v. into the lateral tail vein of syngeneic female mice. All mice are euthanized on day 21 posttransplantation or earlier if the mice seemed moribund. The lungs are removed and weighed, and surface tumor colonies are quantified in a blinded fashion under a dissecting microscope. A 50% hydroxypropyl-β-cyclodextrin solution is prepared; at 20%, this solution serves as the vehicle. AMG487 is added to the 50% solution, and it is incubated in a sonicating water bath for 2 hours with occasional vortexing. Distilled water is added to give the appropriate final concentration of AMG487 in 20% of hydroxypropyl-β-cyclodextrin.

References
M.Wt

603.59

Formula

C₃₂H₂₈F₃N₅O₄

CAS No.

473719-41-4

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 41 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.65% ee.: 99.97%

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Product Name:
AMG 487
Cat. No.:
HY-15319
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