AMG 487
作者：齊岳
發(fā)布時間：2023-09-12
09:09:19
點(diǎn)擊數(shù)：
產(chǎn)品名稱：AMG 487
產(chǎn)品描述：
| 產(chǎn)品描述 | 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. |
| 靶點(diǎn)活性 | 125I-ITAC-CXCR3:8.2 nM, 125I-IP10-CXCR3:8 nM |
| 體外活性 | 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]. |
| 體內(nèi)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]. |
| 分子量 | 603.59 |
| 分子式 | C32H28F3N5O4 |
| CAS No. | 473719-41-4 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 41 mg/mL (67.93 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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