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TBK1/IKKε-IN-5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TBK1/IKKε-IN-5图片
CAS NO:1893397-65-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
TBK1/IKKε-IN-5 (compound 1) 是一种口服有效的TBK1IKKε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 activeTBK1andIKKεdual inhibitor, withIC50values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response toPD-1and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used incancerresearch, especially in tumour immunity[1].

IC50& Target

IC50: 1 nM (TBK1), 5.6 nM (IKKε)[1].

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[1].
TBK1/IKKε-IN-5 effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects[1].

Cell Viability Assay[1]

Cell Line:CD4+ and CD8+ T cells, Jurkat T cell leukemia cells
Concentration:0.001-10 μM
Incubation Time:24 h (for IL-2); 96 h(for IFN-γ)
Result:Enhanced secretion of IL-2 and IFN-γ.
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[1].

Animal Model:Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors)[1].
Dosage:40 mg/kg
Administration:Oral gavage; single daily for 26 days (combine with anti-PD-L1).
Result:Exhibited greater tumor control and longer survival when combined with anti-PD-L1 than used alone of both agents
Induced immunologic memory of CT26 cells in mice when combined with anti-PD-L1.
分子量

513.59

性状

Solid

Formula

C28H31N7O3

CAS 号

1893397-65-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 7.81 mg/mL(15.21 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9471 mL9.7354 mL19.4708 mL
5 mM0.3894 mL1.9471 mL3.8942 mL
10 mM0.1947 mL0.9735 mL1.9471 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。