GSK547

GSK547 (GSK'547) 是受体相互作用的丝氨酸/苏氨酸蛋白激酶 1 (RIPK1) 的高选择性和强效抑制剂，可抑制巨噬细胞介导的胰腺癌适应性免疫耐受。

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库存: 现货

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5mg

￥1625.00

1300.00

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10mg

￥2775.00

2220.00

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25mg

￥5500.00

4400.00

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50mg

￥9175.00

7340.00

- +
100mg

￥14425.00

11540.00

- +

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Background

GSK547, a highly selective and potent RIP1 inhibitor, inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].
GSK547 (0.1-100000 nM; 24 hours) pretreats L929 cells with recombinant TNFα and zVAD at various doses for 30 min, then cell death is induced with an IC50 of 32 nM after 24 hours[1].
GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM)[1].
GSK547 (GSK′547; RIP1i) robustly targets RIP1 in vivo. RIP1 inhibition results in immunogenic macrophage differentiation in pancreatic cancer, leading to adaptive immune activation and tumor protection for pancreatic ductal adenocarcinoma (PDA)[1].
GSK547 (100 mg/kg/day; fed via food-based dosing; 15-50 days) reduces tumor burden and extends survival compared with mice treated with controls or Nec-1s[1].

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