TBK1/IKKε-IN-5|cas:1893397-65-3|西域试剂

TBK1/IKKε-IN-5,99.58%

产品编号：Bellancom-128679| CAS NO：1893397-65-3| 分子式：C₂₈H₃₁N₇O₃| 分子量：513.59

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货号	价格	库存与货期
Bellancom-128679	￥4100.00	杭州北京（现货）
Bellancom-128679	￥6550.00	杭州北京（现货）
Bellancom-128679	￥13100.00	杭州北京（现货）

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TBK1/IKKε-IN-5

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 active TBK1 and IKKε dual inhibitor, with IC₅₀ values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity.

体外研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors).
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors).
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors).
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.

性状

Solid

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式