Network Version
Product Name: | AMG 487 | |
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CAS No.: | 473719-41-4 | |
Cat. No.: | HY-15319 | |
MWt: | 603.59 | |
Formula: | C32H28F3N5O4 | |
Purity : | >98% | |
Solubility: | DMSO : ≥ 41 mg/mL | |
Mechanisms: | Target: Cancer Endocrinology Inflammation/Immunology | |
Biological Activity: | ||
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[1].
IC50 & Target:IC50: 8.0 nM (125I-IP-10 binding to CXCR3), 8.2 nM (125I-ITAC binding to CXCR3)
In Vitro: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)[1]. AMG487 (1 μM) develops into fewer lung metastases, and the lungs are significantly smaller than vehicle-treated lungs[2]. AMG487 abrogates proliferation/survival of C26 tumour cells[3]. 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[1]. AMG487 (5 mg/kg, s.c., twice daily) develops fewer metastases than that in vehicle-treated mice[2]. 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[3]. |
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