Formulation: A crystalline solid
Formal Name: N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)-benzeneacetamide
Purity: ≥98%
Formula Markup: C32H28F3N5O4
Formula Weight: 603,6
Shelf life (days): 1460
CAS Number: 473719-41-4
Notes: AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay).{50088} It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models.{47785} AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).{47786}
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