(S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
性状
Oil
IC50 & Target[1][2]
VHL
体外研究(In Vitro)
(S,R,S)-AHPC-PEG2-C4-Cl uses the VHL ligand. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
参考文献
[1]. Craig Crews, et al. Proteolysis Targeting Chimera Compounds and Methods of Preparing and Using Same. US20170121321A1.[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.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (76.77 mM)Ethanol : 50 mg/mL (76.77 mM; Need ultrasonic)