货号	规格	价格	上海	北京	珠海	重庆	武汉
S87655-1mg买3赠1	99.80%	￥450.00 S87655-1mg ￥450.00 现货（买3赠1）	4 4	-	-	-	-
S87655-5mg买3赠1	99.80%	￥790.00 S87655-5mg ￥790.00 现货（买3赠1）	8 8	-	-	-	-
S87655-10mg买3赠1	99.80%	￥1330.00 S87655-10mg ￥1330.00 现货（买3赠1）	5 5	-	-	-	-
S87655-25mg买3赠1	≥98%	￥2450.00 S87655-25mg ￥2450.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S87655-1mg买3赠1

99.80%

￥450.00

S87655-5mg买3赠1

99.80%

￥790.00

S87655-10mg买3赠1

99.80%

￥1330.00

S87655-25mg买3赠1

≥98%

￥2450.00

货期：2-3天

产品描述：

TBK1/IKKε-IN-5 (compound 1) 是一种 TANK-binding kinase 1 (TBK1) 和 IκB kinase-ε (IKKε/IKK-i) 的双重抑制剂，对于TBK1和IKKε的IC50值分别为1.0 nM和5.6 nM。TBK1 /IKKε被抑制可增强对PD-1阻断的反应，从而有效地预测了体内的肿瘤反应

靶点：

TBK1(Cell-free assay):1.0 nM; IKKε(Cell-free assay):5.6 nM;IκB/IKK

体外研究：

TBK1/IKKε-IN-5(compound 1) effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects, and enhances secretion of IL-2 and IFN-γ 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 TBK1/IKKε-IN-1(compound 1) to PD-1 blockade enhances killing of CT26 MDOTS, associated with decreased levels of CCL4, CCL3, and IL-1β and induction of cytokines involved in activated innate immune responses

体内研究：

Balb/c mice bearing CT26 tumors are treated with TBK1/IKKε-IN-1(compound 1) ± anti-PD-L1. Consistent with MDOTS profiling data, greater tumor control and longer survival is evident with TBK1/IKKε-IN-1(compound 1) + anti-PD-L1 than with either TBK1/IKKε-IN-1(compound 1) or anti-PD-L1 alone. Reimplantation of CT26 into mice with exceptional responses to combination therapy shows no growth, whereas EMT-6 implanted tumors grow normally, suggesting induction of immunologic memory of CT26 cells in mice treated with TBK1/IKKε-IN-1(compound 1) + anti-PD-L1. Therefore, MDOTS profiling effectively recapitulates the in vivo response to PD-1 blockade +/− TBK1/IKKε inhibition, highlighting the potential of ex vivo screening in MDOTS to develop combination immunotherapies.

细胞实验：

Cell lines: HCT116 cells, human CD4+ T cells, human CD8+ T cells Concentrations: 1 μM Incubation Time: 1 h, 24 h, 96 h Method: Interleukin-2 and interferon gamma analysis—Freshly isolated human CD4+ and CD8+ T cells are spun down and resuspended in serum free X-vivo15 media supplemented with 5 ng/mL IL-17 and incubated overnight at 37°C. Cells are plated on anti-CD3 coated plates with 2 μg/mL anti-CD28. Cells are treated in replicate plates with a dose-titration of TBK1/IKKε-IN-1(compound 1) for 24 hours for IL-2 and 96 hours for IFNγ. IL-2 and IFNγ in the supernatant are measured using single-or multi-plex immunoassay. Jurkat T cell leukemia cells plated on anti-CD3 coated plates are treated with a dose titration of TBK1/IKKε-IN-1(compound 1) for 24 hours.

动物实验：

Animal Models: 11-12 week old female Balb/c mice implanted with 1×106 CT26 colon carcinoma cells. Dosages: 40 mg/kg Administration: Oral gavage

参考文献：

1. Russell WJ, et al. Ex Vivo Profiling of PD-1 Blockade Using Organotypic Tumor Spheroids. Cancer Discov. 2018 Feb;8(2):196-215.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.947 ml	9.735 ml	19.471 ml
5 mM	0.389 ml	1.947 ml	3.894 ml
10 mM	0.195 ml	0.974 ml	1.947 ml
50 mM	0.039 ml	0.195 ml	0.389 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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