store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 615 | 现货 | ||
2 mg | ¥ 898 | 现货 | ||
5 mg | ¥ 1,180 | 现货 | ||
10 mg | ¥ 1,680 | 现货 | ||
25 mg | ¥ 3,550 | 现货 | ||
50 mg | ¥ 5,130 | 现货 | ||
100 mg | ¥ 7,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,580 | 现货 |
产品描述 | 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. |
靶点活性 | [125I]-IP10-CXCR3:8 nM, [125I]-ITAC-CXCR3:8.2 nM |
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].
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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].
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分子量 | 603.59 |
分子式 | C32H28F3N5O4 |
CAS No. | 473719-41-4 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41 mg/mL (67.93 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6568 mL | 8.2838 mL | 16.5675 mL | 41.4188 mL |
5 mM | 0.3314 mL | 1.6568 mL | 3.3135 mL | 8.2838 mL | |
10 mM | 0.1657 mL | 0.8284 mL | 1.6568 mL | 4.1419 mL | |
20 mM | 0.0828 mL | 0.4142 mL | 0.8284 mL | 2.0709 mL | |
50 mM | 0.0331 mL | 0.1657 mL | 0.3314 mL | 0.8284 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AMG 487 473719-41-4 Autophagy GPCR/G Protein Immunology/Inflammation CXCR Metastatic metastasis inhibit cancer CXCL11 CXC chemokine receptors CXCL10 chemokine AMG487 AMG-487 receptor CXCR3 Inhibitor Breast colon inhibitor