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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.
Patent. CN111228491B 2022 Jul 01.
Patent. CN111228491B
AMG 487 purchased from AbMole
Patent. CN111228491A 2022-07-01.
Patent. CN111228491A
AMG 487 purchased from AbMole
| 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 |
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