AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
IC50&Target
I-IP10-CXCR3
8 nM (IC50)
I-ITAC-CXCR3
8.2 nM (IC50)
体外研究
AMG 487 inhibits CXCR3-mediated cell migration by the three CXCR3 chemokines (IP-10 IC50=8 nM, ITAC IC50=15 nM, and MIG IC50=36 nM). Furthermore, AMG 487 inhibits calcium mobilization in response to ITAC (IC50=5 nM). AMG487 (1 μM) develops into fewer lung metastases, and the lungs are significantly smaller than vehicle-treated lungs. AMG487 abrogates proliferation/survival of C26 tumour cells.
体内研究
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. AMG487 (5 mg/kg, s.c.)-treated mice exhibits fewer pulmonary nodules than the control mice in both the models. AMG487 reduces the tumour volume.
分子式
C32H28F3N5O4
分子量
603.59
CAS号
473719-41-4
运输条件
Room temperature in continental US; may vary elsewhere.