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TAK-676
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。
TAK-676图片
CAS NO:2553413-93-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
TAK-676 是一种干扰素基因刺激因子激动剂 (STING),触发STING信号通路激活和 I 型干扰素激活。TAK-676 也是一种免疫系统调节剂,具有完全消退和持久记忆的 T 细胞免疫功能。TAK-676 能够促进持久的干扰素依赖性抗肿瘤免疫反应。
生物活性

TAK-676 is an agonist ofSTING, triggering the activation ofSTINGsignaling pathway andtype I interferons. TAK-676 is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. TAK-676 promotes durable IFN-dependent antitumor immunity[1].

IC50& Target

STING, Type I interferons[1]

体外研究
(In Vitro)

TAK-676 (1.1, 3.3, and 10 μM; 2 h) dose-dependently activates the STING-TBK1-IRF3 pathway in THP1-Dual human AML cells and CT26.WT cells, but is critically dependent on STING expression[1].
TAK-676 (0-1 μM; 24 h) exerts in vitro immune cell activation function in mouse BM-derived dendritic cells in a dose-dependent manner[1].
TAK-676 (0-1 μM; 24 h) promotes the activation of dendritic cells (DC), natural killer (NK) cells, and T cells, with activation EC50s of 1.27 μM (MoDC), 0.32 μM (BMDC), 0.271 μM (NK), 0.216 μM (CD8+), 0.249 μM (CD4+) at 24 h, respectively[1].

Western Blot Analysis[1]

Cell Line:THP1-Dual human AML cells and CT26.WT cells
Concentration:1.1, 3.3, 10 μM
Incubation Time:2 hours
Result:Increased pTBK1, pSTING, pIRF3 protein level in a dose-dependent manner.
Not induced the phosphorylation of pTBK1 (S172) or pIRF3 (S396) in the absence of STING expression.
体内研究
(In Vivo)

TAK-676 (0.025-2 mg/kg; i.v.; single dose) is well tolerated, exhibits dose-proportional pharmacokinetics in plasma, and exhibits higher exposure in tumor in mice[1].
TAK-676 (1 mg/kg/d, 2 mg/kg/d; i.v.; 13 d) shows anti-tumor function on BALB/c mice bearing A20 syngeneic tumors/CT26.WT syngeneic tumors mode[1].

Animal Model:BALB/c mice bearing A20 syngeneic tumors/CT26.WT syngeneic tumors model[1]
Dosage:1 or 2 mg/kg/day
Administration:Intravenous injection; for 3, 6, 9, 12 day, respectively
Result:Resulted in significant T cell–dependent in vivo antitumor activity.
Induced dose-dependent cytokine responses and increased the activation and proliferation of immune cells within the TME and tumor-associated lymphoid tissue.
Clinical Trial
分子量

754.48

Formula

C21H20F2N8Na2O10P2S2

CAS 号

2553413-93-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.