| Identification | Back Directory | [Name]
AMG 487 | [CAS]
473719-41-4 | [Synonyms]
AMG 487
N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)benzeneacetamide
Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)- | [Molecular Formula]
C32H28F3N5O4 | [MOL File]
473719-41-4.mol | [Molecular Weight]
603.59 |
| Chemical Properties | Back Directory | [Melting point ]
161.2℃ (ethyl acetate heptane ) | [storage temp. ]
Keep in dark place,Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO:41.0(Max Conc. mg/mL);67.93(Max Conc. mM) | [form ]
A crystalline solid | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)benzeneacetamide is a selective and potent antagonist of the chemokine receptor CXCR3. | [Biological Activity]
AMG 487 is an orally availablepotent 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) th at 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.). | [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]. | [IC 50]
125I-IP10-CXCR3: 8 nM (IC50); 125I-ITAC-CXCR3: 8.2 nM (IC50) | [storage]
Store at -20°C |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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