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- CAS号：
473719-41-4
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥466.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥1200.0 |
| 规格： | 5mg | 产品价格： | ￥896.0 |
| 规格： | 10mg | 产品价格： | ￥1272.0 |
| 规格： | 25mg | 产品价格： | ￥2696.0 |
| 规格： | 50mg | 产品价格： | ￥3896.0 |
| 规格： | 100mg | 产品价格： | ￥5536.0 |
| 规格： | 200mg | 产品价格： | ￥7464.0 |
Product Introduction
Bioactivity
| 名称 | AMG 487 |
| 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. |
| 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]. |
| 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]. |
| 存储条件 | Store at low temperature,Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.31 mM), Sonication is recommended. DMSO : 41 mg/mL (67.93 mM), Sonication is recommended. |
| 关键字 | receptor | Metastatic | metastasis | Inhibitor | inhibit | CXCR3 | CXCR | CXCL11 | CXCL10 | CXC chemokine receptors | colon | chemokine | cancer | Breast | AMG-487 | AMG487 | AMG 487 | 125I-ITAC-CXCR3 | 125I-IP10-CXCR3 |
| 相关产品 | Soquelitinib | Nicotinamide N-oxide | Plerixafor octahydrochloride | Tanimilast | rac-NBI-74330 | Tannic acid | CXCR2-IN-1 | Kynurenic acid | Artemotil | AZD8309 | CXCL-CXCR1/2-IN-1 | 3-Indoleglyoxylic acid |
| 相关库 | Inhibitor Library | Angiogenesis related Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Autophagy Compound Library | ReFRAME Related Library | Fluorochemical Library | NO PAINS Compound Library | GPCR Compound Library | Membrane Protein-targeted Compound Library | Immunology/Inflammation Compound Library |
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相关实验
水平的水分转运的活性。氟化钠是一种磷脂酶抑制剂，加上 EGTA 和 EDTA，减少磷脂活性。Leupeptin 是一种蛋白酶抑制剂。抗坏血酸是一种抗氧化剂，二硫苏糖醇是一种巯基保护剂。聚乙烯吡咯烷酮（PVP ) 被加入以吸附酚类化合物。组成见表 11-1。 ( 3 ) 微粒缓冲液：微粒体颗粒悬浮在一种与分相方案兼容的缓冲液中。成分如表 11-2所示。 ( 4 ) 分离相：用于 PM 分离的 2 个聚体分别是葡聚糖 T-500 和聚乙二醇 3350，6.4 (m/m) 。两相系统也含有
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化合物 AMG 487【473719-41-4】
￥466 - 7464
