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SML3153

Sigma-Aldrich

AMG 487

≥98% (HPLC)

Sinónimos:

(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-trifluoromethoxyphenyl)-acetamide, AMG-487, AMG487

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About This Item

Fórmula empírica (notación de Hill):
C32H28F3N5O4
Número de CAS:
473719-41-4
Peso molecular:
603.59
MDL number:
MFCD30536209
UNSPSC Code:
12352200
NACRES:
NA.51

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

AMG 487 is an orally available, potent and selective chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8/8.2 nM against CXCL10/11 (IP-10/ITAC) for CXCR3 binding) that inhibits CXCR3 ligands-induced cell migration (CXCL10/11/9 IC50 = 8/15/36 nM). AMG 487 inhibits ITAC-induced calcium mobilization in vitro (IC50 = 5 nM) and reduces bleomycin-induced cellular lung recruitment in wild-type mice to the same level as in Cxcr3-deficient mice in vivo (3 mg/kg b.i.d. s.c.).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

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BMC Immunology, 22(1), 3-3 (2021)
Tonya C Walser et al.
Cancer research, 66(15), 7701-7707 (2006-08-04)
Tumor cells aberrantly express chemokines and/or chemokine receptors, and some may promote tumor growth and metastasis. We examined the expression and function of chemokine receptor CXCR3 in a syngeneic murine model of metastatic breast cancer. By flow cytometry, CXCR3 was
Ming-Xia Zhu et al.
Experimental cell research, 397(2), 112365-112365 (2020-11-17)
Mantle cell lymphoma (MCL) is a unique subtype of B-cell non-Hodgkin lymphoma with a generally aggressive and heterogeneous clinical course. Chemokines are one of the complex components in the tumor microenvironment (TME), and they play a vital role in tumor
Michael Johnson et al.
Bioorganic & medicinal chemistry letters, 17(12), 3339-3343 (2007-04-24)
A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a (125)I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using
Jin Qian et al.
Cell communication and signaling : CCS, 19(1), 9-9 (2021-01-23)
To investigate the effect of lactic acid (LA) on the progression of bone metastasis from colorectal cancer (CRC) and its regulatory effects on primary CD115 (+) osteoclast (OC) precursors. The BrdU assay, Annexin-V/PI assay, TRAP staining and immunofluorescence were performed
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