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AMG 487

Cat. No. M9070
AMG 487 Structure
Size Price Availability
5mg USD 144  USD160 4-7 Days
10mg USD 216  USD240 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AMG 487 prevents the chemokines I-IP-10 and I-ITAC from binding to CXCR3. In the cellular assays, AMG 487 inhibits CXCR3-mediated cell migration with IC50 values of 8nM, 15nM and 36nM for I-IP-10, I-ITAC and MIG, respectively.

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. AMG487 (5 mg/kg, s.c., twice daily) develops fewer metastases than that in vehicle-treated mice.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 603.59
Formula C32H28F3N5O4
CAS Number 473719-41-4
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C

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.
Henne KR, et al. Drug Metab Dispos. 2012 Jul;40(7):1429-40. PMID: 22517972.

Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism.
Cambien B, et al. Br J Cancer. 2009 Jun 2;100(11):1755-64. PMID: 19436305.

Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer.
Walser TC, et al. Cancer Res. 2006 Aug 1;66(15):7701-7. PMID: 16885372.

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Keywords: AMG 487 supplier, CXCR, inhibitors

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