Powder: -20°C for 3 years | In solvent: -80°C for 2 years
NAV-2729 是有效的Arf1/Arf6活化抑制剂。
产品描述 | NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6. |
体外活性 | NAV-2729(25 μM) inhibits spontaneous nucleotide exchange of Δ13Arf6 by ~15%. NAV-2729 inhibits the activation of Δ13Arf6 by BRAG2Sec7PH by 25%. Δ17Arf1 has no measurable spontaneous nucleotide exchange. Activation of Δ17Arf1 by BRAG2Sec7PH is inhibited by NAV-2729, and the efficiency is markedly higher than that for Arf6 (50%). In a dose-response experiment, nucleotide exchange rates are reduced by 50% by 10 μM NAV-2729 for Δ17Arf1 while 50% inhibition is not achieved even at 25 μM NAV-2729 for Δ13Arf6[1]. NAV-2729 blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6 and spontaneous activation of Arf6 and its activation by cytohesins and BRAG. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell[1]. NAV-2729 is more effective toward Arf1 than Arf6[1]. |
体内活性 | In orthotopic xenograft mouse model of uveal melanoma, systemic treatment of NAV-2729 interfere with tumorigenesis and tumor growth[2]. |
分子量 | 456.88 |
分子式 | C25H17ClN4O3 |
CAS No. | 419547-11-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 50 mg/mL (109.44 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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。
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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。
NAV-2729 419547-11-8 GPCR/G Protein Others GTPase Inhibitor inhibit NAV2729 NAV 2729 inhibitor