1807530-05-7

Usage

Uses

Used in Pharmaceutical Industry:
Hydroxy-PEG5-t-butyl acetate is used as a solubility enhancer for hydrophobic drugs, improving their dissolution and bioavailability in aqueous media. The hydrophilic PEG chain increases the solubility of the drug, facilitating its absorption and distribution within the body.
Used in Drug Delivery Systems:
Hydroxy-PEG5-t-butyl acetate is used as a component in the design of drug delivery systems, such as nanoparticles or liposomes. The PEG chain can provide stealth properties, reducing the clearance rate and extending the circulation time of the drug delivery system. Additionally, the hydroxyl group allows for the attachment of targeting ligands or other functional groups to improve the specificity and efficacy of the drug delivery.
Used in Chemical Synthesis:
Hydroxy-PEG5-t-butyl acetate is used as an intermediate in the synthesis of various PEGylated compounds. The hydroxyl group can be further derivatized or replaced with other reactive functional groups, enabling the creation of a wide range of PEG-based molecules with diverse applications in research, medicine, and other industries.
Used in Bioconjugation:
Hydroxy-PEG5-t-butyl acetate is used as a linker in bioconjugation processes, where it can be used to attach biologically active molecules, such as peptides, proteins, or nucleic acids, to other molecules or surfaces. The PEG chain can provide stability and solubility to the conjugate, while the hydroxyl and t-butyl protected carboxyl groups offer sites for attachment and subsequent deprotection to reveal reactive groups for further modification.

Upstream product

• 4792-15-8 Pentaethylene glycol 
• 1807537-31-0 tert-butyl 1-phenyl-2,5,8,11,14,17-hexaoxanonadecan-19-oate 
• 57671-28-0 2-(2-{2-[2-(2-benzyloxyethoxy)ethoxy]ethoxy}ethoxy)ethanol 
• 5292-43-3 bromoacetic acid tert-butyl ester 

Downstream Products

• 1448451-72-6 tert-butyl 17-azido-3,6,9,12,15-pentaoxaheptadecan-1-oate 

Relevant academic research and scientific papers

Protein degradation through covalent inhibitor-based PROTACs

Tremendous advancements in proteolysis targeting chimera (PROTAC) technology have been made in recent years. However, whether a covalent inhibitor-based PROTAC can be developed remains controversial. Here, we successfully developed chimeric degraders based on covalent inhibitors to degrade BTK and BLK kinases, demonstrating that covalent inhibitor-based PROTACs are viable and useful tools.

MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

ANTI-EGFR ANTIBODY DRUG CONJUGATES

The invention relates to anti-Epidermal Growth Factor Receptor (EGFR) antibody drug conjugates (ADCs) which inhibit Bcl-xL, including compositions and methods of using said ADCs.

SMALL MOLECULES

Compounds having the general structure A - L - B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1 B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.

Identification and Characterization of von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted degraders is still relatively young, the potential for this modality to become a differentiated and therapeutic reality is strong, such that both academic and pharmaceutical institutions are now entering this interesting area of research. In this article, we describe a broadly applicable process for identifying degrader hits based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) and have generalized the key structural elements associated with degradation activities. Compound 3i is a potent hit (TBK1 DC50 = 12 nM, Dmax = 96%) with excellent selectivity against a related kinase IKK?, which was further used as a chemical tool to assess TBK1 as a target in mutant K-Ras cancer cells.

RAF-DEGRADING CONJUGATE COMPOUNDS

The present disclosure provides, inter alia, RAF-Degrading Conjugate Compounds that are useful in the treatment of cancer and other RAF related diseases. Also provided are, pharmaceutical compositions, methods of treatment, and kits comprising a RAF- Degrading Conjugate Compound.

ANTI-CD98 ANTIBODIES AND ANTIBODY DRUG CONJUGATES

The invention relates to anti-CD98 antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

ANTI-CD98 ANTIBODIES AND ANTIBODY DRUG CONJUGATES

The invention relates to anti-CD98 antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

ANTI-B7-H3 ANTIBODIES AND ANTIBODY DRUG CONJUGATES

The invention relates to B7 homology 3 protein (B7-H3) antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

ANTIBODY DRUG CONJUGATES WITH CELL PERMEABLE BCL-XL INHIBITORS

Small molecule Bcl-xL inhibitors and Antibody Drug Conjugates (ADCs) comprising small molecule Bcl-xL inhibitors are disclosed herein. The Bcl-xL inhibitors and ADCs of the disclosure are useful for, among other things, inhibiting anti-apoptotic Bcl xL proteins as a therapeutic approach towards the treatment of diseases that involve a dysregulated apoptosis pathway.