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NAV-2729

目录号: PL08499 纯度: ≥98%

NAV-2729 是一种 Arf1/Arf6 活化抑制剂。

CAS No. :419547-11-8

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中文名称	NAV-2729
英文名称	NAV-2729
英文别名	NAV-2729;2-benzyl-3-(4-chlorophenyl)-5-(4-nitrophenyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one;NAV 2729;2-benzyl-3-(4-chlorophenyl)-5-(4-nitrophenyl)-1H-pyrazolo[1,5-a]pyrimidin-7-one;3-(4-Chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one;Oprea1_305395;NAV2729;AMY23749;BDBM50168142;D80454;2-benzyl-3-(4-chlorophenyl)-5-(4-nitrop
Cas No.	419547-11-8
分子式	C₂₅H₁₇ClN₄O₃
分子量	456.88
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	NAV-2729 是一种 Arf1/Arf6 活化抑制剂。

产品详情	NAV-2729 是一种 Arf1/Arf6 活化抑制剂。
生物活性	NAV-2729 is a dual Arf1/Arf6 activation inhibitor.
性状	Solid
IC50 & Target[1][2]	Arf6 Arf1
体外研究(In Vitro)	NAV-2729 directly binds to Arf6. Based on a structural homology model of the Arf6/Arf6-GEF complex, it is predicted that NAV-2729 associates with Arf6 at the Arf6 GEF-binding area, which is distinct from the guanine nucleotide-binding pocket of Arf6. NAV-2729 blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell. NAV-2729 is a dual Arf1/Arf6 inhibitor and is more effective toward Arf1 than Arf6. NAV-2729 blocks spontaneous activation of Arf6 and its activation by cytohesins and BRAG. NAV-2729 is an inhibitor of the spontaneous activation of Arf6, and it also inhibits the activation of Arf6 by its GEFs, ARNO and BRAG2, in solution. The inhibitory profile of NAV-2729 is analyzed at a concentration of 25 μM, which is reported to result in almost total inhib
体内研究(In Vivo)	Systemic treatment of mice with NAV-2729 interfere with tumorigenesis and tumor growth in orthotopic xenograft mouse model of uveal melanoma. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Yamauchi Y, et al. Machineries regulating the activity of the small GTPase Arf6 in cancer cells are potential targets for developing innovative anti-cancer drugs. Adv Biol Regul. 2017 Jan;63:115-121. [2]. Benabdi S, et al. Family-wide Analysis of the Inhibition of Arf Guanine Nucleotide Exchange Factors with Small Molecules: Evidence of Unique Inhibitory Profiles. Biochemistry. 2017 Sep 26;56(38):5125-5133.

溶解度数据	In Vitro: DMSO : 50 mg/mL (109.44 mM; Need ultrasonic)配制储备液

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[1]. Yamauchi Y, et al. Machineries regulating the activity of the small GTPase Arf6 in cancer cells are potential targets for developing innovative anti-cancer drugs. Adv Biol Regul. 2017 Jan;63:115-121.
[2]. Benabdi S, et al. Family-wide Analysis of the Inhibition of Arf Guanine Nucleotide Exchange Factors with Small Molecules: Evidence of Unique Inhibitory Profiles. Biochemistry. 2017 Sep 26;56(38):5125-5133.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

NAV-2729

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