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AMG 487

AMG 487 是可口服的选择性趋化因子受体3拮抗剂，对 I-IP-10、I-ITAC 和 MIG 的 IC50 值分别为 8、15 和 36nM。

CAS号

473719-41-4

分子式

C32H28F3N5O4

主要靶点

CXCR

仅限科研使用

Cat No : CM03603

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Synonyms

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  • CAS No.: 473719-41-4

    AMG 487
    CAS#: 473719-41-4

产品信息

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

CAS号 473719-41-4
分子式 C32H28F3N5O4
主要靶点 CXCR
主要通路 G蛋白偶联受体|免疫与炎症|自噬
分子量 603.59
纯度 99.88%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

125I-ITAC-CXCR3:8.2 nM|125I-IP10-CXCR3:8 nM

体内活性

AMG487, a small molecular weight antagonist. In vivo, systemic CXCR3 antagonism by preventive or curative treatments with AMG487 markedly inhibited the implantation and the growth of human and mouse CRC cells within lung without affecting that in the liver. In addition, we measured increased levels of CXCR3 and ligands expression within lung nodules compared with liver tumours. Activation of CXCR3 receptors by its cognate ligands facilitates the implantation and the progression of CRC cells within lung tissues and that inhibition of this axis decreases pulmonary metastasis of CRC in two murine tumour models[3].

体外活性

AMG487 is a small molecular weight antagonist of CXCR3. 66.1 tumor cells were pretreated with AMG487 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 AMG487 also inhibited experimental lung metastasis. In contrast to the antimetastatic effect of AMG487, local growth of 66.1 mammary tumors was not affected by receptor antagonism. Murine mammary tumor cells express CXCR3 which facilitates the development of lung metastases.Indicate for the first time that a small molecular weight antagonist of CXCR3 has the potential to inhibit tumor metastasis[2].

溶解度

DMSO:41 mg/mL (67.93 mM)

参考文献

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.
4.Henne KR, et al. Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. Drug Metab Dispos. 2012 Jul;40(7):142

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