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Submit Review(±)-AMG 487 is an antagonist of CXCR3; inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 (IC50 values are 8.0 and 8.2 nM respectively). Inhibits CXCR3-mediated cell migration by the chemokines IP-10, ITAC and MiG in vitro (IC50 values are 8, 15 and 36 nM respectively). Also shown to inhibit lung metastasis in a mouse model of metastatic breast cancer.
This product is racemic.
(±)-AMG 487 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 603.59 |
公式 | C32H28F3N5O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 947536-03-0 |
PubChem ID | 10282265 |
InChI Key | WQTKNBPCJKRYPA-UHFFFAOYSA-N |
Smiles | CCOC(C=C3)=CC=C3N2C(C1=CC=CN=C1N=C2C(N(CC4=CC=CN=C4)C(CC5=CC=C(OC(F)(F)F)C=C5)=O)C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 60.36 | 100 |
以下数据基于产品分子量 603.59。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.66 mL | 8.28 mL | 16.57 mL |
5 mM | 0.33 mL | 1.66 mL | 3.31 mL |
10 mM | 0.17 mL | 0.83 mL | 1.66 mL |
50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
参考文献是支持产品生物活性的出版物。
Johnson et al (2007) Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg.Med.Chem.Lett. 17 3339 PMID: 17448658
Walser et al (2006) Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 66 7701 PMID: 16885372
Cambien et al (2009) Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br.J.Cancer 100 1755 PMID: 19436305
If you know of a relevant reference for (±)-AMG 487, please let us know.
关键词: (±)-AMG 487, (±)-AMG 487 supplier, CXCR3, chemokine, receptors, antagonists, inhibitors, inhibits, cell, migration, metastasis, ±-AMG487, ±-AMG_487, Chemokine, CXC, Receptors, 4487, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (±)-AMG 487 的部分引用包括:
Gordón-Alonso et al (2017) Galectin-3 captures IF.-gamma in the tumor matrix reducing chemokine gradient production and T-cell tumor infiltration. Nat Commun 8 793 PMID: 28986561
Hitoo et al (2021) Wnt signaling enhances macrophage responses to IL-4 and promotes resolution of atherosclerosis. Elife 10 PMID: 33720008
Karsten et al (2019) Neutrophils promote CXCR3-dependent itch in the development of atopic dermatitis. Elife 8 PMID: 31631836
Tsunaki et al (2020) Metastasis-initiating cells induce and exploit a fibroblast niche to fuel malignant colonization of the lungs. Nat Commun 11 1494 PMID: 32198421
Guo et al (2018) Interleukin-1β induces CXCR3-mediated chemotaxis to promote umbilical cord mesenchymal stem cell transendothelial migration. Stem Cell Res Ther. 9 281 PMID: 30359318
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I used this product to reduce the activated CXCR3+ T cells in mouse with chronic interstitial cystitis.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.