AMG 487
- Product Name
- AMG 487
- CAS No.
- 473719-41-4
- Chemical Name
- AMG 487
- Synonyms
- AMG 487;AMG 487 - Bio-X ?;AMG 487, 10 mM in DMSO;N-[(1R)-1-[3-(4-ethoxyphenyl)-4-oxoquinazolin-2-yl]ethyl]-N-(pyridin-2-ylmethyl)-2-[4-(trifluoromethoxy)phenyl]acetamide - [AC79904];N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)benzeneacetamide;(R)-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;Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)-;Metastatic,metastasis,inhibit,cancer,CXCL11,CXC chemokine receptors,AMG-487,AMG487,CXCL10,chemokine,receptor,CXCR3,AMG 487,CXCR,Inhibitor,Breast,colon
- CBNumber
- CB32627318
- Molecular Formula
- C32H28F3N5O4
- Formula Weight
- 603.59
- MOL File
- 473719-41-4.mol
AMG 487 Property
- 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
N-Bromosuccinimide Price
- Product number
- SML3153
- Product name
- AMG 487
- Purity
- ≥98% (HPLC)
- Packaging
- 10MG
- Price
- $98.1
- Updated
- 2026/03/19
- Product number
- SML3153
- Product name
- AMG 487
- Purity
- ≥98% (HPLC)
- Packaging
- 50MG
- Price
- $394
- Updated
- 2026/03/19
- Product number
- 28416
- Product name
- AMG 487
- Packaging
- 1mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 28416
- Product name
- AMG 487
- Packaging
- 25mg
- Price
- $684
- Updated
- 2024/03/01
- Product number
- 28416
- Product name
- AMG 487
- Packaging
- 5mg
- Price
- $179
- Updated
- 2024/03/01
AMG 487 Chemical Properties,Usage,Production
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 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) 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)
AMG 487 Preparation Products And Raw materials
Raw materials
Preparation Products
AMG 487 Suppliers
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