Related Products of 17696-11-6. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). Author is Zhang, Hao; Zhao, Hong-Yi; Xi, Xiao-Xiao; Liu, Yan-Jie; Xin, Minhang; Mao, Shuai; Zhang, Jun-Jie; Lu, A-Xin; Zhang, San-Qi.
Herein, the discovery of small mol. EGFR degraders based on the proteolysis targeting chimera (PROTAC) strategy was reported. In the present study, 13 EGFR degraders containing pyrido[3,4-d]pyrimidine moiety I [X = CH2C(O)NHCH2CH2C(O), CH2CH2CH2CH2C(O), CH2CH2CH2CH2CH2C(O), etc.], II [C = CH2C(O)NHCH2CH2C(O), CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2C(O), CH2CH2OCH2CH2OCH2CH2, CH2CH2CH2CH2CH2CH2C(O), etc.] were designed and synthesized. Promising PROTACs I [X = CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2CH2CH2C(O)] induced degradation of EGFR in HCC827 cells with the DC50 values of 45.2 and 34.8 nM, resp. Cellular protein-controlling machinery ubiquitin proteasome system (UPS) was involved in the degradation process. Furthermore, the degraders I [X = CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2CH2CH2C(O)] could significantly induce the apoptosis of HCC827 cells and arrest the cells in G1 phase. These findings demonstrated that compounds I [X = CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2CH2CH2C(O)] could serve as effective EGFRdel19-targeting degraders in HCC827 cells. v.
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Bromide – Wikipedia,
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