AMG 487 |
| カタログ番号GC11939 |
AMG 487は、経口投与可能な選択的なケモカイン受容体3（CXCR3）拮抗薬であり、CXCR3に対するCXCL10およびCXCL11の結合をそれぞれ8.0および8.2 nMのIC50値で阻害する。
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Cas No.: 473719-41-4
Sample solution is provided at 25 µL, 10mM.
AMG 487 is an oral, selective chemokine receptor 3 (CXCR3) antagonist that inhibits CXCL10 and CXCL11 binding to CXCR3 with IC50 values of 8.0 and 8.2 nM, respectively[1].
AMG 487(1 µM AMG 487;18 h (C26 cells) or 40 h (HT29 cells)), the CXCR3 antagonist, significantly inhibited the migratory responses of the cells to each of the three ligands(rCXCL9, rCXCL10 and rCXCL11)[2].
the AMG 487-treated mice(SCID mice:1 µM AMG 487;s.c.7-17day. Balb/c mice:5 mg/kg: s.c.˙twice daily.) exhibited fewer pulmonary nodules than the control mice in both the models: a 62% reduction in the human mode and 42% less nodules in the mouse model. The inhibitory effect of AMG 487 treatment was also detectable in the cumulative tumour volume with a reduction by 58% in the lungs of the HT29-injected immunodeficient mice and by 51% in the lungs of the C26-injected syngeneic mice[2]. During in vitro differentiation, the addition of AMG 487(3- 60µM) decreased the expression of DC co-stimulatory markers, indicating that DC was in a semi-mature state[4]. 66.1 tumor cells were pretreated with AMG 487 prior to i.v. injection into immune-competent female mice. Antagonism of CXCR3 on 66.1 tumor cells inhibited experimental lung metastasis, and this antimetastatic activity was compromised in mice depleted of natural killer cells. Systemic administration of AMG 487(5 mg/kg;s.c.;twice daily) also inhibited experimental lung metastasis[3]. In mice, injection of AMG-487 (i.c.v.)significantly attenuated the accumulation of c-fos in neurons induced by polyinosinic-polycytidylic acid (PIC)[5]. WT mice treated with AMG-487 (5 µg/g twice a day) showed a 45% reduction in bone loss and decreased osteoclasts after LPS injections[6]. Meanwhile, AMG 487 treatment significantly reduced bone loss in mice[7].
References:
[1]. Johnson M, Li AR,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. doi: 10.1016/j.bmcl.2007.03.106. Epub 2007 Apr 6. PMID: 17448658.
[2]. Cambien B, Karimdjee BF, et,al. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br J Cancer. 2009 Jun 2;100(11):1755-64. doi: 10.1038/sj.bjc.6605078. Epub 2009 May 12. PMID: 19436305; PMCID: PMC2695685.
[3]. Walser TC, Rifat S, 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. doi: 10.1158/0008-5472.CAN-06-0709. PMID: 16885372.
[4]. Qin C, Liu H, et,al.In Vitro Immunological Effects of CXCR3 Inhibitor AMG487 on Dendritic Cells. Arch Immunol Ther Exp (Warsz). 2020 Apr 1;68(2):11. doi: 10.1007/s00005-020-00577-3. PMID: 32239302.
[5]. Petrisko TJ, Konat GW. Peripheral viral challenge increases c-fos level in cerebral neurons. Metab Brain Dis. 2021 Oct;36(7):1995-2002. doi: 10.1007/s11011-021-00819-z. Epub 2021 Aug 18. PMID: 34406561.
[6]. Hiyari S, Green E, et,al. Genomewide Association Study Identifies Cxcl Family Members as Partial Mediators of LPS-Induced Periodontitis. J Bone Miner Res. 2018 Aug;33(8):1450-1463. doi: 10.1002/jbmr.3440. Epub 2018 May 22. PMID: 29637625; PMCID: PMC8434897.
[7]. Lari S, Hiyari S, et,al. Local delivery of a CXCR3 antagonist decreases the progression of bone resorption induced by LPS injection in a murine model. Clin Oral Investig. 2022 Aug;26(8):5163-5169. doi: 10.1007/s00784-022-04484-z. Epub 2022 Apr 25. PMID: 35462591; PMCID: PMC9710470.
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