TBK1/IKKε-IN-5

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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。

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 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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	1.9471 mL	9.7354 mL	19.4708 mL
5 mM	0.3894 mL	1.9471 mL	3.8942 mL
10 mM	0.1947 mL	0.9735 mL	1.9471 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。