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ES-072是一种口服选择性EGFR突变体(EGFR-T790M)抑制剂,主要通过抑制EGFR-T790M活性并激活GSK3α工作。通过这一途径,该化合物使PD-L1在Ser279和Ser283位点发生磷酸化,进一步促进E3泛素连接酶ARIH1对PD-L1的招募,从而标记其进行泛素化和蛋白酶体介导的降解。此作用机制既抑制了癌细胞生长,也通过降低PD-L1水平来加强抗肿瘤免疫响应。因此,ES-072对于抑制非小细胞肺癌细胞(NSCLC)的增殖具有显著效果。
ES-072是一种口服选择性EGFR突变体(EGFR-T790M)抑制剂,主要通过抑制EGFR-T790M活性并激活GSK3α工作。通过这一途径,该化合物使PD-L1在Ser279和Ser283位点发生磷酸化,进一步促进E3泛素连接酶ARIH1对PD-L1的招募,从而标记其进行泛素化和蛋白酶体介导的降解。此作用机制既抑制了癌细胞生长,也通过降低PD-L1水平来加强抗肿瘤免疫响应。因此,ES-072对于抑制非小细胞肺癌细胞(NSCLC)的增殖具有显著效果。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells. |
分子量 | 528.53 |
分子式 | C25H27F3N8O2 |
CAS No. | 2089721-94-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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