产品说明书
GSK547
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同义名 : | GSK'547 |
| CAS号 : | 2226735-55-1 | |
| 货号 : | A1145742 | |
| 分子式 : | C20H18F2N6O | |
| 纯度 : | 99%+ | |
| 分子量 : | 396.393 | |
| MDL号 : | MFCD32062767 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 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] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.61mL 2.52mL 1.26mL |
25.23mL 5.05mL 2.52mL |
| 参考文献 |
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