MSX-122
分子式：C16H16N6分子量：292.34

简介：MSX-122是一种新型的CXCR4部分拮抗剂，IC50约为10 nM。
物理性状及指标：
外观：……………………粉末
溶解性：…………………H2O ：Insoluble；Ethanol：Insoluble；DMSO: 3 mg/mL (10.26 mM)
含量：……………………>98%
储存温度：-20℃，避光防潮密闭干燥

生物活性

描述

MSX-122是一种新型的CXCR4部分拮抗剂，IC50约为10 nM。

IC50& Target

CXCR4

~10 nM

体外

MSX-122 is also incapable of blocking the binding of 125I-labeled CXCL12 to CXCR4. MSX-122 appears to be insufficiently large to block all binding sites between CXCR4 and CXCL12. MSX-122 blocks certain CXCR4 functions via binding to the CXCL12-binding site and interfering with CXCR4/CXCL12-mediated signaling. MSX-122 can intervene in the Gαi-signaling pathway (cAMP modulation), but not the Gq-pathway (calcium flux)

体内

MSX-122 blocks bleomycin-induced lung fibrosis involving chemotaxis and homing of CXCR4-positive mesenchymal progenitor cells into the lungs. MSX-122 exhibits anti-inflammatory activity in a carrageenan-induced paw edema model. MSX-122 blocks lung metastasis of breast cancer and SCCHN, and liver metastasis of uveal melanoma in vivo.

细胞实验

Cell lines:MDA-MB-231 cells
Concentrations:1, 10, 100, and 1000 nM
Incubation Time:15 mins
Method:

For binding affinity assay, MDA-MB-231 cells cultured in an 8-well slide chamber are preincubated with MSX-122 at 1, 10, 100, and 1000 nM. Then the cells are fixed with 4% formaldehyde and incubated with 50 nM biotinylated TN14003, and followed by Rhodamine staining.
(Only for Reference)

动物实验

Animal Models:Male C57BL/6 mice (age 5–6 weeks)
Formulation:dissolved in 10% DMSO and 45% 2-hydroxypropyl-β cyclodextrin
Dosages:10 mg/kg
Administration:i.p. injection
(Only for Reference)

储液配置及储存：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。

浓度/体积/质量	1 mg	5 mg	10 mg
1 mM	3.4207 mL	17.1034 mL	34.2067 mL
5 mM	0.6841 mL	3.4207 mL	6.8413 mL
10 mM	0.3421 mL	1.7103 mL	3.4207 mL

【注意】
●我司产品为非无菌包装，若用于细胞培养，请提前做预处理，除去热原细菌，否则会导致染菌。

●部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，以上数据仅供参考交流研究之用。

规格	5mg

MSX-122

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