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| Bioactivity |
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]. |
| Invitro |
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]. |
| Name |
AMG 487 |
| CAS |
473719-41-4 |
| Formula |
C32H28F3N5O4 |
| Molar Mass |
603.59 |
| Appearance |
Solid |
| Transport |
Room temperature in continental US; may vary elsewhere. |
| Storage |
| Powder |
-20°C |
3 years |
|
4°C |
2 years |
| In solvent |
-80°C |
6 months |
|
-20°C |
1 month |
|
| Reference |
[1]. Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. [2]. Walser TC, et al. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 2006 Aug 1;66(15):7701-7. [3]. Cambien B, et al. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br J Cancer. 2009 Jun 2;100(11):1755-64. |
