133803-81-3

Usage

Uses

Used in Pharmaceutical Industry:
Hydroxy-PEG3-t-butylester is used as an ADC (Antibody Drug Conjugate) linker for the synthesis of antibody drug conjugates. This application takes advantage of its ability to connect antibodies with cytotoxic drugs, enhancing the targeting of cancer cells and improving the therapeutic index of the treatment.
Used in Chemical Synthesis:
Hydroxy-PEG3-t-butylester is used as a PROTAC (Proteolysis Targeting Chimera) linker for the synthesis of protein degradation inducers. Its role in this application is to connect a target protein ligand with an E3 ubiquitin ligase ligand, promoting the degradation of specific proteins and offering a new approach to treating various diseases, including cancer.
Used in Drug Delivery Systems:
Hydroxy-PEG3-t-butylester is used as a solubility enhancer in drug delivery systems due to its hydrophilic PEG spacer. This property can improve the pharmacokinetics and biodistribution of therapeutic agents, potentially reducing side effects and increasing the efficacy of the treatment.
Used in Bioconjugation:
Hydroxy-PEG3-t-butylester is used as a versatile building block in bioconjugation, allowing for the attachment of various biomolecules, such as peptides, proteins, or other functional groups, to create novel bioconjugates with tailored properties and applications in research and therapeutics.

in vitro

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.

Upstream product

• 1663-39-4 tert-Butyl acrylate 
• 112-27-6 2,2'-[1,2-ethanediylbis(oxy)]bisethanol 
• 111-46-6 diethylene glycol 

Downstream Products

• 1271728-79-0 tert-butyl 3-(2-(2-azidoethoxy)ethoxy)propanoate 
• 1312309-63-9 3-(2-(2-azidoethoxy)ethoxy)propanoic acid 
• 1379649-80-5 ethyl 3-(2-(2-hydroxyethoxy)ethoxy)propanoate 
• 1379649-81-6 ethyl 3-(2-(2-(tosyloxy)ethoxy)ethoxy)propanoate 
• 1379649-73-6 3-(2-(2-mercaptoethoxy)ethoxy)propanoic acid 
• 1609643-83-5 perfluorophenyl 3-(2-(2-(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)ethoxy)ethoxy)propanoate 
• 756525-95-8 2-methyl-2-propanyl 3-[2-(2-aminoethoxy)ethoxy]propanoate 
• 756525-98-1 3-(2-{2-[3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanamido]ethoxy}ethoxy)propanoic acid 
• 1037589-69-7 3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-N-{2-[2-(3-oxo-3-{4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]phenylamino}propoxy)ethoxy]ethyl}propanamide 
• 850090-14-1 3-{2-[2-(4-{2-[2-(2-tert-butoxycarbonyl-ethoxy)-ethoxy]-ethoxy}-2,5-diiodo-phenoxy)-ethoxy]-ethoxy}-propionic acid tert-butyl ester 
• 796062-74-3 2,5-bis(9-carboxy-3,6-dioxaoctyloxy)-1,4-diiodobenzene 
• 850090-13-0 9-(p-toluenesulfonyloxy)-3,6-diocanonanoic acid tert-butyl ester 
• 1807503-92-9 3-[2-(2-bromoethoxy)ethoxy]propanoic acid 

Relevant academic research and scientific papers

Efficient synthesis of polyethylene glycol mono-carboxylate via Michael conjugate addition

Poly(ethylene glycol) (PEG) with one carboxylate group, the very useful precursors for the synthesis of the PEG derived heterobifunctional linkers, are synthesized in high yield in one-pot via Michael conjugate addition of acrylate esters with PEG and catalyst amount of sodium in THF.

Synthesis of novel heterobifunctional isocyanato cross-linkers and their applications for the preparation of 10-hydroxycamptothecin and SN-38 conjugates with melanotransferrin p97

Novel heterobifunctional cross-linkers with an isocyanato group, a protected carboxylic group, and a linear chain spacer are synthesized in high yield by coupling monofunctionalized PEG with 1,6-diisocyanatohexane. The isocyanato groups of those linkers are highly reactive and are efficient reagents to couple with the hydroxy groups of 10-hydroxycamptothecin and SN-38 under mild conditions to give a useful precursor for the synthesis of their bioconjugates with proteins such as melanotransferrin p97. Copyright Taylor & Francis Group, LLC.

Synthesis of 6-O-benzyl guanine and its conjugations with linkers

An improved synthesis of 6-O-benzyl guanine which is an important inhibitor of O6-alkyl-guanine DNA alkyltransferase (AGT) is described. In addition the conjugation of this guanine derivative was achieved with a functionalised hydrophilic linke

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

The receptor tyrosine kinase FLT-3 is frequently mutated in acute myeloid leukemia; however, current small molecule inhibitors suffer from limited efficacy in the clinic. Conversion of a FLT-3 inhibitor (quizartinib) into a proteolysis targeting chimera (

New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone-cycloalkyne click reaction

We report the first pretargeting in vivo study using the Strain-Promoted Sydnone-Alkyne Cycloaadition (SPSAC) reaction. The injection of a fluorine-18 labeled cyclooctyne three days after cetuximab bearing chlorosydnone moieties allowed a significant detection of the tumor by PET imaging suggesting an efficient click reaction inside the tumoral site. With a kinetic constant superior to 300 M-1 s-1, the SPSAC reaction might be an interesting tool, in addition to tetrazine-cyclooctene ligation, for in vivo chemistry.

NOVEL CONNECTED BODY AND USE THEREOF IN SPECIFIC CONJUGATION BETWEEN BIOMOLECULE AND DRUG

PROBLEM TO BE SOLVED: To provide: a method for producing a connected body; a method for using the connected body in the production of a uniform conjugate; and a method for applying the conjugate in the treatment of cancer, infectious diseases, and autoimmune diseases. SOLUTION: A novel connected body is provided that includes a 2,3-di-substituted succinic acid group or a 2-mono-substituted or 2,3-di-substituted fumaric acid or maleic acid (trans (E)- or cis (Z)-butenedioic acid) group for conjugating 2 or more compounds/cytotoxic agents per connected body with a cell-binding molecule by specifically bridge-linking to a pair of thiol on the cell-binding molecule. The connected body is exemplified by the following general formula. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

Synthesis of KUE-siRNA Conjugates for Prostate Cancer Cell-Targeted Gene Silencing

The delivery of siRNAs to selectively target cells poses a great challenge in RNAi-based cancer therapy. The lack of suitable cell-targeting methods seriously restricts the advance in delivering siRNAs to extrahepatic tissues. Based on prostate-specific m

PCSK9 ANTAGONIST COMPOUNDS

Disclosed are compounds of Formula (A), or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula (I) or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.

PCSK9 ANTAGONIST COMPOUNDS

Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof: (I) wherein A, A1, A2, R1, R2 and R3 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.

Conjugate and preparation method and application thereof

The invention relates to the technical field of biology, and discloses a conjugate and a preparation method and application thereof. The conjugate is formed by covalent attachment of a nitrogen-azide modified targeting ligand and a propargyl-modified smal