产品描述
(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
体外活性
(S,R,S)-AHPC-PEG2-C4-Cl uses the VHL ligand[1]. The linker is 6-2-2. 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-PEG2-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.
1835705-57-1
分子式
C32H47ClN4O6S
分子量
651.26
别名
VH032-PEG2-C4-Cl;VHL Ligand-Linker Conjugates 7;E3 ligase Ligand-Linker Conjugates 10
储存和溶解度
DMSO:50 mg/mL (76.77 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years