TBK1/IKKε-IN-5|1893397-65-3|-陌孚医药/Medlife

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TBK1/IKKε-IN-5

目录号: PL02953 纯度: ≥99%

CAS No. :1893397-65-3

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中文名称	TBK1/IKKε-IN-5
中文别名	2-(氧杂-4-基氧基)-5-[4-[4-[4-(氧杂环丁-3-基)哌嗪-1-基]苯胺基]-1,3,5-三嗪-2-基]苄腈
英文名称	TBK1/IKKε-IN-5
英文别名	TBK1/IKKepsilon-IN-5;BDBM277845;TBK1/IKK;A-IN-1(compound 1);US10040781, Example 67;s8922;5-(4-((4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)amino)-1,3,5-triazin-2-yl)-2-((tetrahydro-2H-pyran-4-yl)oxy)benzonitrile;2-(oxan-4-yloxy)-5-[4-[4-[4- (oxetan-3-yl)piperazin-1- yl]anilino]-1,3,5-triazin-2- yl]benzonitrile;2-(Oxan-4-yloxy)-5-[4-[4-[4-(oxetan-3-yl)piperazin-1-yl]anilino]-1,3,5-triazin-2-yl]benzonitrile;TBK1/IKKε-IN-5
Cas No.	1893397-65-3
分子式	C₂₈H₃₁N₇O₃
分子量	513.59
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TBK1/IKKε-IN-5 (compound 1) 是一种口服有效的 TBK1 和 IKKε 的双重抑制剂，其 IC₅₀ 值分别为 1 nM 和 5.6 nM。TBK1/IKKε-IN-5 能增强对 PD-1 的阻断反应，与 anti-PD-L1 联用时能诱导大鼠的免疫记忆。TBK1/IKKε-IN-5 可用于癌症，尤其是肿瘤免疫的研究。
生物活性	TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC 50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity.
性状	Solid
IC50 & Target[1][2]	IC50: 1 nM (TBK1), 5.6 nM (IKKε).
体外研究(In Vitro)	TBK1/IKKε-IN-5 (0.001-10 μM; 24 or 96 h) promotess secretion of IL-2 and IFN-γ in purified CD4+ and CD8+ T cells and IL-2 in Jurkat human T-cell leukemia cells. TBK1/IKKε-IN-5 effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)	TBK1/IKKε-IN-5 (40 mg/kg; p.o.; single daily for 26 days) shows good antitumor activity and prolongs survival, as well as induces immunologic memory of CT26 cells in mice when combines with anti-PD-L1. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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]. Jenkins RW, et al. Ex Vivo Profiling of PD-1 Blockade Using Organotypic Tumor Spheroids. Cancer Discov. 2018 Feb;8(2):196-215.

溶解度数据	In Vitro: DMSO : 7.81 mg/mL (15.21 mM; Need ultrasonic)配制储备液

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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。

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