518044-31-0

Usage

Uses

Used in Pharmaceutical Industry:
Hydroxy-PEG3-t-butyl acetate is used as a molecular building block for the development of drug conjugates and prodrugs. The hydrophilic PEG spacer improves the solubility and pharmacokinetic properties of the resulting drug molecules, while the hydroxyl and t-butyl protected carboxyl groups facilitate chemical modifications and conjugation to therapeutic agents.
Used in Bioconjugation and Chemical Synthesis:
Hydroxy-PEG3-t-butyl acetate serves as a versatile intermediate for the synthesis of bioconjugates, such as PEGylated proteins, peptides, and other biomolecules. The hydroxyl group allows for the attachment of various functional groups, while the t-butyl protected carboxyl group can be deprotected under acidic conditions to enable further reactions.
Used in Drug Delivery Systems:
In the field of drug delivery, Hydroxy-PEG3-t-butyl acetate is used as a component in the design of targeted drug delivery systems. The PEG spacer can be utilized to improve the solubility and circulation time of drug-loaded nanoparticles or liposomes, while the functional groups enable the attachment of targeting ligands or other therapeutic agents.
Used in Diagnostics and Imaging:
Hydroxy-PEG3-t-butyl acetate can be employed in the development of contrast agents for medical imaging techniques, such as magnetic resonance imaging (MRI) or computed tomography (CT). The hydrophilic PEG spacer and functional groups can be used to enhance the stability and biocompatibility of imaging agents, while the t-butyl protected carboxyl group allows for the incorporation of imaging moieties.
Used in Cosmetics and Personal Care:
In the cosmetics and personal care industry, Hydroxy-PEG3-t-butyl acetate is used as an ingredient in the formulation of skin care and hair care products. The hydrophilic PEG spacer improves the solubility and skin permeation of active ingredients, while the hydroxyl and t-butyl protected carboxyl groups enable the creation of stable emulsions and gels.

Upstream product

• 5292-43-3 bromoacetic acid tert-butyl ester 
• 112-27-6 2,2'-[1,2-ethanediylbis(oxy)]bisethanol 
• 55489-58-2 triethylene glycol monobenzyl ether 
• 1443467-88-6 1-phenyl-2,5,8,11-tetraoxatridecan-13-oic acid tert-butyl ester 

Downstream Products

• 1530778-24-5 t-butyl [2-(2-{2-[(4-methylbenzene-1-sulfonyl)oxy]ethoxy}ethoxy)ethoxy]acetate 
• 1618678-46-8 (2S,4R)-1-((S)-2-(tert-butyl)-20-((7R,8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)-15-methyl-4-oxo-6,9,12-trioxa-3,15-diazaicosan-1-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide 
• 1618678-45-7 (2S,4R)-1-((S)-2-(tert-butyl)-14-(4-(5-((7R,8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)pentyl)piperazin-1-yl)-4-oxo-6,9,12-trioxa-3-azatetradecan-1-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide 
• 883564-93-0 13,13-dimethyl-11-oxo-3,6,9,12-tetraoxatetradecan-1-oic acid 

Relevant academic research and scientific papers

Compound targeting ubiquitination degradation tyrosinase as well as preparation method and application thereof

A Tyr inhibitor kojic acid is covalently bound to a pomalidomide or VHL enzyme targeting ligand through a linkage chain to obtain a specific structure, and the preparation method is simple to operate and mild in condition. The generation of melanin is inhibited, the anti-melanin tumor effect is remarkable, and the safety period of vegetables and fruits can be remarkably prolonged. The compound targeted ubiquitination degradation tyrosinase provided by the invention has wide application prospects in medicine, food and cosmetics.

Di-substituted maleic amide linker for antibody drug conjugating and preparation method and use thereof

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule thro

Functionalized 2-Hydroxybenzaldehyde-PEG Modules as Portable Tags for the Engagement of Protein Lysine ?-Amino Groups

The formation of reversible-covalent interactions between a small-molecule ligand and its protein target is emerging as a general strategy to design binders with increased affinity. In this context, 2-hydroxybenzaldehyde (2HB) has been recently proposed a

Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma

Traditional EZH2 inhibitors are developed to suppress the enzymatic methylation activity, and they may have therapeutic limitations due to the nonenzymatic functions of EZH2 in cancer development. Here, we report proteolysis-target chimera (PROTAC)-based EZH2 degraders to target the whole EZH2 in lymphoma. Two series of EZH2 degraders were designed and synthesized to hijack E3 ligase systems containing either von Hippel-Lindau (VHL) or cereblon (CRBN), and some VHL-based compounds were able to mediate EZH2 degradation. Two best degraders, YM181 and YM281, induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clinically used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degraders displayed promising antitumor activities in lymphoma xenografts and patient-derived primary lymphoma cells. Our study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma.

Heterocyclic compound and application thereof

The invention discloses a heterocyclic compound and application thereof. The invention provides a heterocyclic compound as shown in a formula I, or pharmaceutically acceptable salt thereof. The heterocyclic compound can be used for degrading ALK, c-Met and ROS proteins.

PROTEOLYSIS TARGETING CHIMERIC (PROTAC) COMPOUND WITH E3 UBIQUITIN LIGASE BINDING ACTIVITY AND TARGETING ALPHA-SYNUCLEIN PROTEIN FOR TREATING NEURODEGENERATIVE DISEASES

The present disclosure relates to bifunctional compounds, which find utility as modulators of alpha-synuclein (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 or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. Such diseases or disorders are alpha-synucleinopathies or neurodegenerative diseases associated with alpha-synuclein accumulation and aggregation, such as e.g. Parkinson Disease, Alzheimer's Disease, dementia, dementia with Lewy bodies or multiple system atrophy, in particular Parkinson's Disease.

POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES

The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the 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 RAF, 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 or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

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.

Compound for targeted degradation of ALK, c-Met and ROS1 proteins, and preparation method thereof

The invention provides a novel compound for targeted degradation of ALK, c-Met and ROS1 proteins, wherein the compound is represented by a formula A, is formed by linking an ubiquitin ligase E3 recognition ligand and an ALK, c-Met and ROS1 protein inhibitor compound through a linking arm, and can selectively induce degradation of ALK, c-Met and ROS1 proteins and mutant proteins of the ALK, c-Met and ROS1 proteins. According to the invention, a bifunctional small molecule is obtained; and in-vitro anti-tumor activity data of the compound show that the compound has high-efficiency anti-tumor activity on conventional tumor cells, has strong inhibition activity on mutant cell strains (BaF3/EML4-ALKG1202R, BaF3/EML4-ALKL1196M and BaF3-TEL-ALK-C1156Y) causing the drug resistance, provides a effective antitumor drug for clinical application, has great application value, brings good news for tumor treatment, especially for some drug-resistant patients, and has important social benefits.

AMIDE COMPOUND HAVING BET PROTEOLYSIS-INDUCING ACTION AND MEDICINAL APPLICATION THEREOF

The present invention aims to provide a compound that: has an excellent cytotoxic action on cancer cells, excellent induction of BET protein degradation in cancer cells, and an excellent binding-inhibiting action on BET protein and acetylated histone; and is effective as an anti-cancer agent, a BET protein degradation-inducing agent, or a BET protein inhibiting agent. A compound indicated in general formula (I) or a pharmacologically acceptable salt thereof. {In the formula, each symbol is as outlined in the Description.}