CAS NO: | 1835705-55-9 |
规格: | 98% |
分子量: | 751.42 |
包装 | 价格(元) |
100mg | 电议 |
500mg | 电议 |
1g | 电议 |
2g | 电议 |
Background:
E3 ligase Ligand-Linker Conjugates 8 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
E3 ligase Ligand-Linker Conjugates 8 uses the cereblon ligand[1]. The linker is 6-2-2-6. The linkers contain a mixture of hydrophobic and hydrophilic moieties to balance the hydrophobicity/hydrophilicity of the resulting hybrid compounds. PROTACs that induce the degradation of an oncogenic tyrosine kinase, BCR-ABL has been developed. E3 ligase Ligand-Linker Conjugates 8 can be attached to potent TKIs (bosutinib and dasatinib) that mediate the degradation of c-ABL and BCR-ABL by hijacking either CRBN or VHL E3 ubiquitin ligase [2].
[1]. US 20170121321 A1 [2]. Lai AC, et al. Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL. Angew Chem Int Ed Engl. 2016 Jan 11;55(2):807-10.