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Signaling Pathway

AMG 487

HY-15319

(AMG487; AMG-487)

AMG 487

AMG 487 Chemical Structure

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).

Size Price Stock Quantity
10 mM * 1 mL in DMSO $465 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €456 In-stock
5 mg €343 In-stock
10 mg €490 In-stock
50 mg €1470 In-stock
100 mg €2058 In-stock
200 mg Get quote
500 mg Get quote

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Product name: AMG 487
Cat. No.: HY-15319

AMG 487 Data Sheet

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    DataSheet

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Related Compound Libraries

Biological Activity of AMG 487

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 [1]
Target: CXCR3
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)) [4].
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 [2]. 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 [3].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 603.59 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C32H28F3N5O4
CAS No 473719-41-4
Solvent & Solubility

Soluble to 100 mM in DMSO

Preparing Stock Solutions

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

References on AMG 487

Inhibitor Kit

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