Computed Properties of C11H21BrO2. 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: 11-Bromoundecanoic acid, is researched, Molecular C11H21BrO2, CAS is 2834-05-1, about Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation. Author is Jiang, Liang; Wang, Yuting; Li, Qian; Tu, Zhengchao; Zhu, Sihua; Tu, Sanfang; Zhang, Zhang; Ding, Ke; Lu, Xiaoyun.
Bcr-Abl threonine 315 to isoleucine 315 (T315I) gatekeeper mutation induced drug resistance remains an unmet clin. challenge for the treatment of chronic myeloid leukemia (CML). Chem. degradation of Bcr-AblT315I protein has become a potential strategy to overcome drug resistance. Herein, we first described the design, synthesis, and evaluation of a new class of selective Bcr-AblT315I proteolysis-targeting chimeric (PROTAC) degraders based on GZD824 (reported as Bcr-AblT315I inhibitor by our group). One of the degrader 7o with 6-member carbon chain linkage with pomalidomide exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nmol/L, resp., and has an IC50 value of 26.8 ± 9.7 nmol/L against Ba/F3T315I cells. Further, 7o also displays substantial tumor regression against Ba/F3-Bcr-AblT315I xenograft model in vivo.
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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI