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AMG 487 Chemical Structure
|Product name: AMG 487|
|Cat. No.: HY-15319|
AMG 487 is a small molecule antagonist of the chemokine receptor CXCR3; inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 (IC50 values are 8.0 and 8.2 nM respectively).
IC50 value: 8 nM 
in vitro: Although in vitro activity loss assays failed to demonstrate CYP3A4 time-dependent inhibition (TDI) with AMG 487, its M2 phenol metabolite readily produced TDI when remaining activity was assessed using either midazolam or testosterone (K(I) = 0.73-0.74 μM, k(inact) = 0.088-0.099 min(-1)) .
in vivo: 66.1 tumor cells were pretreated with AMG487 prior to i.v. injection into immune-competent female mice. Antagonism of CXCR3 on 66.1 tumor cells inhibited experimental lung metastasis, and this antimetastatic activity was compromised in mice depleted of natural killer cells. Systemic administration of AMG487 also inhibited experimental lung metastasis . In vivo, systemic CXCR3 antagonism by preventive or curative treatments with AMG487 markedly inhibited the implantation and the growth of human and mouse CRC cells within lung without affecting that in the liver. In addition, we measured increased levels of CXCR3 and ligands expression within lung nodules compared with liver tumours .
|M.Wt||603.59||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
Soluble to 100 mM in DMSO
|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|
. Henne KR, et al. Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. Drug Metab Dispos. 2012 Jul;40(7):1429-40.
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