Description
(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.
Product information
CAS Number: 1835705-57-1
Molecular Weight: 651.26
Formula: C32H47ClN4O6S
Chemical Name: (2S,4R)-1-[(2S)-2-(2-{2-[(6-chlorohexyl)oxy]ethoxy}acetamido)-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide
Smiles: CC1N=CSC=1C1C=CC(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCCCCCCl)C(C)(C)C)=CC=1
InChiKey: VVGFRQKHZOZAAG-UWPQIUOOSA-N
InChi: InChI=1S/C32H47ClN4O6S/c1-22-28(44-21-35-22)24-11-9-23(10-12-24)18-34-30(40)26-17-25(38)19-37(26)31(41)29(32(2,3)4)36-27(39)20-43-16-15-42-14-8-6-5-7-13-33/h9-12,21,25-26,29,38H,5-8,13-20H2,1-4H3,(H,34,40)(H,36,39)/t25-,26+,29-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 50 mg/mL (76.77 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
(S,R,S)-AHPC-PEG2-C4-Cl uses the VHL ligand. 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.
Products are for research use only. Not for human use.
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