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CAS No.: 2550393-21-8
MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib. MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. It is bioavailable in mice following ip administration.
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实验方案
技术信息
CAS号 | 2550393-21-8 | 储存条件 |
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分子式 | C46H54ClFN8O8 | 运输 | 蓝冰 | |
分子量 | 901.42 | 别名 |
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