Xie, Shaowen; Sun, Yuan; Liu, Yulin; Li, Xinnan; Li, Xinuo; Zhong, Wenyi; Zhan, Feiyan; Zhu, Jingjie; Yao, Hong; Yang, Dong-Hua; Chen, Zhe-Sheng; Xu, Jinyi; Xu, Shengtao published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK)》.Computed Properties of C11H24N2O2 The article contains the following contents:
A series of novel anaplastic lymphoma kinase (ALK) degraders were designed and synthesized based on proteolysis-targeting chimera (PROTAC) technol. by linking two alectinib analogs (I and II) with pomalidomide through linkers of different lengths and types. The most promising degrader III possessed a high ALK-binding affinity and potent antiproliferative activity in the ALK-dependent cell lines and did not exhibit obvious cytotoxicity in ALK fusion-neg. cells. More importantly, the efficacy of compound III in a Karpas 299 xenograft mouse model was further evaluated based on its ALK-sustained degradation ability in vivo. The reduction in tumor weight in the compound III-treated group (10 mg/kg/day, I.V.) reached 75.82%, while alectinib reduced tumor weight by 63.82% at a dose of 20 mg/kg/day (P.O.). Taken together, our findings suggest that alectinib-based PROTACs associated with the degradation of ALK may have promising beneficial effects for treating ALK-driven malignancies. The experimental process involved the reaction of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Computed Properties of C11H24N2O2)
N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Computed Properties of C11H24N2O2
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