产品描述
(S,R,S)-AHPC-C6-PEG3-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
体外活性
(S,R,S)-AHPC-C6-PEG3-C4-Cl 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. (S,R,S)-AHPC-C6-PEG3-C4-Cl 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].
Cas No.
1835705-55-9
分子式
C38H59ClN4O7S
分子量
751.42
别名
VH032-C6-PEG3-C4-Cl;E3 ligase Ligand-Linker Conjugates 8;VHL Ligand-Linker Conjugates 12;(S,R,S)-AHPC-C6-PEG3-C4-Cl
储存和溶解度
DMSO:100 mg/mL (133.08 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years