TBK1/IKKε-IN-1(compound 1)

For research use only. Not for use in humans.

目录号:S8922

TBK1/IKKε-IN-1(compound 1) Chemical Structure

CAS No. 1893397-65-3

TBK1/IKKε-IN-5 (compound 1) 是一种 TANK-binding kinase 1 (TBK1) 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。

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RMB 10787.1 现货
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产品安全说明书

IκB/IKK抑制剂选择性比较

生物活性

产品描述 TBK1/IKKε-IN-5 (compound 1) 是一种 TANK-binding kinase 1 (TBK1) 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 [1]
(Cell-free assay)
IKKε [1]
(Cell-free assay)
1.0 nM 5.6 nM
体外研究

TBK1/IKKε-IN-1(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.[1]

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.[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • 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.


    (Only for Reference)
动物实验:

[1]

- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 10 mg/mL (19.47 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 513.59
化学式

C28H31N7O3

CAS号 1893397-65-3
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID