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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
SIAIS039 is an orally active c-ros oncogene 1 (ROS1) -specific PROTAC with DC 50 s of 154.46nM, 126.47nM, 143.69nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis , and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib , a linker EM-12 , and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib ; Blue: VHL ligand; Black: linker).