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GSK547 {[allProObj[0].p_purity_real_show]}

货号:A1145742 同义名: GSK'547

GSK'547 is a highly selective and potent RIP1 inhibitor with improved oral bioavailability.

GSK547 化学结构 CAS号:2226735-55-1
GSK547 化学结构
CAS号:2226735-55-1
GSK547 3D分子结构
CAS号:2226735-55-1
GSK547 化学结构 CAS号:2226735-55-1
GSK547 3D分子结构 CAS号:2226735-55-1
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GSK547 纯度/质量文件 产品仅供科研

货号:A1145742 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 NF-κB 其他靶点 纯度
PDTC ammonium 98%
QNZ ++++

NF-κB, IC50: 11 nM

99%+
Sodium 4-Aminosalicylate Dihydrate 98%
Sodium Salicylate 95%
Parthenolide p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

98%
Phenethyl caffeate 98%
Andrographolide 98+%
Curcumin Nrf2,HDAC 98%
SC75741 +++

NF-κB, EC50: 200 nM

99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

GSK547 生物活性

描述 GSK'547 is a highly selective and potent RIP1 inhibitor with improved oral bioavailability. Administration of GSK'547 exhibited protective effect against pancreatic ductal adenocarcinoma and liver metastasesin vivo, reducing tumor burden and extending survival, accompanied with increased pan-T cell infiltration and the CD8/CD4 ratio, as well as T cell activation. This tumor protection mediated by GSK'547 is synergistic with PD-1 blockade and inducible co-stimulator agonism. Also, inhibition of RIP1 by GSK'547 activated innate and adaptive immunity and decreased tumor viability in organotypic models of human pancreatic ductal adenocarcinoma. GSK'547 induced M1-like programming and upregulated STAT1 signaling in BMDM. Inhibition of RIP1 by GSK'547 enhanced the capacity of TAMs to induce immunogenic CD4+ T cell differentiation in vitro.
作用机制 GSK'547 binds in an allosteric pocket between the N-terminal and C-terminal domains at the back of the ATP binding site of RIP1 kinase.[1]

GSK547 动物研究

Dose Mice: 100 mg/kg[1] (p.o.), 0.01 mg/kg - 10 mg/kg[1] (WT Mice, p.o.)
Administration p.o.

GSK547 参考文献

[1]Wang W, Marinis JM, et al. RIP1 Kinase Drives Macrophage-Mediated Adaptive Immune Tolerance in Pancreatic Cancer. Cancer Cell. 2018 Nov 12;34(5):757-774.e7.

GSK547 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.23mL

5.05mL

2.52mL

GSK547 技术信息

CAS号2226735-55-1
分子式C20H18F2N6O
分子量 396.393
别名 GSK'547
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 250 mg/mL(630.69 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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