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TBK1/IKKε-IN-5

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Chemical Structure| 1893397-65-3 同义名 : compound 1
CAS号 : 1893397-65-3
货号 : A1177218
分子式 : C28H31N7O3
纯度 : 99%+
分子量 : 513.591
MDL号 : MFCD32067990
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 6 mg/mL(11.68 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
动物实验配方：
生物活性
描述 TBK1/IKKε inhibition can enhance response to PD-1 blockade, which effectively predicts tumor response in vivo. QUN97653 is a novel potent and selective TBK1/IKKε dual inhibitor with IC50s of 1 nM and 5.6 nM for TBK1 and IKKε, respectively. QUN97653 effectively blocked immune suppressive cytokine elaboration by CT26 cell line spheroids and enhanced secretion of IFN-γ and IL-2 from purified CD4+ and CD8+ T cells from healthy human donors and IL-2 from Jurkat human T-cell leukemia cells. Ex vivo addition of QUN97653 to PD-1 blockade enhanced killing of CT26 MDOTS (murine-derived organotypic tumor spheroids), associated with decreased levels of CCL4, CCL3, and IL-1β and induction of cytokines involved in activated innate immune responses. In Balb/c mice bearing CT26 tumors, greater tumor control and longer survival was evident with combination of QUN97653 with anti-PD-L1 than with either QUN97653 or anti-PD-L1 alone[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.47mL

3.89mL

1.95mL
参考文献

[1]Jenkins RW, Aref AR, Lizotte PH, et al. Ex Vivo Profiling of PD-1 Blockade Using Organotypic Tumor Spheroids. Cancer Discov. 2018;8(2):196-215