AMG 487

SKU: orb1310006

Description

AMG 487 is a selective small molecule CXCR3 antagonist, potently blocking CXCL10 and CXCL11 binding with IC50 values of approximately 8 nM. It is widely used in research to investigate the role of CXCR3 in autoimmune diseases, transplant rejection, and cancer biology, employing both in vitro binding assays and in vivo disease models.

Research Area

Cell Biology, Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 473719-41-4
• MW: 603.59
• Purity: 99.89% (May vary between batches)
• Formula: C₃₂H₂₈F₃N₅O₄
• SMILES: CCOc1ccc(cc1)-n1c(nc2ncccc2c1=O)[C@@H](C)N(Cc1cccnc1)C(=O)Cc1ccc(OC(F)(F)F)cc1
• Target: CXCR
• Solubility: DMSO:41 mg/mL (67.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.31 mM)

Bioactivity

• Target IC50:
  [125I]-ITAC-CXCR3:8.2 nM|[125I]-IP10-CXCR3:8 nM
• In Vivo:
  AMG487, a small molecular weight antagonist. 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. Activation of CXCR3 receptors by its cognate ligands facilitates the implantation and the progression of CRC cells within lung tissues and that inhibition of this axis decreases pulmonary metastasis of CRC in two murine tumour models.
  Read more...
• In Vitro:
  AMG487 is a small molecular weight antagonist of CXCR3. 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 contrast to the antimetastatic effect of AMG487, local growth of 66.1 mammary tumors was not affected by receptor antagonism. Murine mammary tumor cells express CXCR3 which facilitates the development of lung metastases.Indicate for the first time that a small molecular weight antagonist of CXCR3 has the potential to inhibit tumor metastasis.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

receptor, cancer, 125I-IP10-CXCR3, 125I-ITAC-CXCR3, AMG 487, AMG487, AMG-487, colon, Breast, chemokine, CXCR3, CXCR, CXC chemokine receptors, CXCL11, CXCL10, Metastatic, metastasis, inhibit, Inhibitor

Compound Identifiers

PubChem CID

24957182