产品说明书
NAV-2729
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同义名 : | Grassofermata |
| CAS号 : | 419547-11-8 | |
| 货号 : | A691659 | |
| 分子式 : | C25H17ClN4O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 456.88 | |
| MDL号 : | MFCD01455625 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(109.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | ARF6 (GTPase ADP-ribosylation factor 6) can be activated by a variety of different ARF-guanine nucleotide exchange factors (ARF-GEFs), depending on the stimulating factor or cell type and is an attractive candidate as an effector of Gαq signaling. NAV-2729 is allosteric, non-nucleotide-competitive and reversible ARF6-selective inhibitor with IC50 value of 1.5μM. NAV-2729 directly inhibited ARF6 as evidenced by nearly equipotent inhibitory effects toward spontaneous and ARF-GEF-catalyzed ARF6 nucleotide exchange. Treatment of Mel92.1 and Mel202 cells with NAV-2729 at concentration of 10μM inhibited ARF6 activation, as well as mimicked ARF6 and GEP100 knockdown by driving GNAQ from the cytoplasmic vesicles to the plasma membrane and reducing anchorage-independent colony growth. NAV-2729 also blocked all of the known downstream signaling pathways of oncogenic GNAQ, including PLC/PKC, Rho/Rac, YAP, and β-catenin. Administration of NAV-2729 at dose of 30mg/kg, i.p., daily, reduced uveal melanoma cell proliferation and tumorigenesis in a mouse model[2]. | ||
| 作用机制 | NAV-2729 targets ARF6 GEF-binding region.[2] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.19mL 0.44mL 0.22mL |
10.94mL 2.19mL 1.09mL |
21.89mL 4.38mL 2.19mL |
| 参考文献 |
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