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AMG 487 prevents the chemokines I-IP-10 and I-ITAC from binding to CXCR3, it inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50 values of 8.0 and 8.2 nM, respectively. 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.
| Molecular Weight | 603.59 |
| Formula | C32H28F3N5O4 |
| CAS Number | 473719-41-4 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CXCR Products |
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| Elubrixin
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. |
| VUF 11222
VUF 11222 is a CXCR3 non-peptide-like agonist. |
| (±)-AMG 487
(±)-AMG 487 is a racemate of AMG 487. |
| Elubrixin tosylate
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. |
| Elubrixin hydrochloride
Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. |
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Products are for research use only. Not for human use. We do not sell to patients.
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