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(±)-AMG 487

Catalog No.GC15045

CXCR3 antagonist

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(±)-AMG 487 Chemical Structure

Cas No.: 473719-41-4

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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

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Background

AMG 487 is described here instead of (±)-AMG 487. AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) [1]. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG with IC50 values of 8, 15 and 36 nM, respectively [2].

CXCR3, a chemokine receptor, is primarily expressed on activated CD4+ and CD8+ T cells with a Th1 phenotype. It is also expressed on B cells, malignant T cells, natural killer (NK) cells and astrocytes. Its ligands are Mig (CXCL9), IP-10 (CXCL10), and ITAC (CXCL11). These ligands are primarily induced by IFN-γ. CXCR3 and its ligands had been implicated in many inflammatory diseases including inflammatory bowel diseases, rheumatoid arthritis, psoriasis, multiple sclerosis, and transplant rejection [2].

AMG487 blocked in vitro lymphocyte migration mediated by CXCL9, CXCL10 or CXCL11. AMG487 did not affect the proliferation of 66.1 tumor cells at 24, 48 or 72 hours under normal or serum-free growth conditions. It did inhibit the migration of the tumor cells to CXCL9 by 70% [3].

In the lungs of mice, treatment with bleomycin via intra-tracheal instillation after tracheostomy induced cellular recruitment into the lungs. All but the lowest dose AMG 487 treatment group showed significant decrease in cellular infiltration into the lungs (p < 0.005 as determined by Student’s t-test). Subcutaneously administration with AMG 487 at 3 mg/kg twice daily showed migration inhibition results similar to those of CXCR3 deficient mice (n = 8-12 mice per group) [2]. The highly malignant murine mammary tumor cell line 66.1 was pretreated with AMG 487 and hence i.v. injected into immune-competent female mice. AMG487 showed inhibitory effect on experimental lung metastasis [3].

References:
[1].  Tonn GR, Wong SG, Wong SC, et al. An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl) -4-oxo-3,4-
dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.  Drug Metabolism and Disposition, 2009, 37(3): 502-513.
[2].  Johnson M, Li AR, Liu J, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorganic & medicinal chemistry letters, 2007, 17(12): 3339-3343.
[3].  Walser TC, Rifat S, Ma X, et al. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer research, 2006, 66(15): 7701-7707.

Chemical Properties

Cas No. 473719-41-4 SDF
Chemical Name N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-N-(pyridin-3-ylmethyl)-2-(4-(trifluoromethoxy)phenyl)acetamide
Canonical SMILES CCOC1=CC=C(N2C(C(N(C(CC3=CC=C(OC(F)(F)F)C=C3)=O)CC4=CN=CC=C4)C)=NC5=C(C2=O)C=CC=N5)C=C1
Formula C32H28F3N5O4 M.Wt 603.59
Solubility <60.36mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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