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CAS No.: 2226735-55-1

Synonyms: RIP1i;GSK'547

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

规格	价格	促销价格	库存	数量

400-920-2911

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400-920-2911

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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]
动物研究
剂量
Mice: 100 mg/kg^[1] (p.o.), 0.01 mg/kg - 10 mg/kg^[1] (WT Mice, p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 100 mg/kg^[1] (p.o.), 0.01 mg/kg - 10 mg/kg^[1] (WT Mice, p.o.)
给药途径	p.o.

实验方案

技术信息

CAS号	2226735-55-1	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C20H18F2N6O	运输	蓝冰
分子量	396.39	别名	RIP1i;GSK'547

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