872340-65-3

Usage

Uses

Used in Pharmaceutical Industry:
AMINO-PEG12-T-BUTYL ESTER is used as a versatile linker for drug conjugation and development. Its reactivity with various functional groups allows for the attachment of therapeutic agents to PEG chains, enhancing the solubility, stability, and bioavailability of the drug molecules.
Used in Chemical Synthesis:
In the field of chemical synthesis, AMINO-PEG12-T-BUTYL ESTER serves as a key intermediate for the creation of complex PEGylated molecules. The ability to selectively deprotect the t-butyl group enables precise control over the structure and function of the final product.
Used in Bioconjugation:
AMINO-PEG12-T-BUTYL ESTER is utilized as a bioconjugation agent to attach biologically active molecules, such as peptides, proteins, or nucleic acids, to PEG chains. This process can improve the pharmacokinetic properties of these biomolecules, extending their circulation time in the body and reducing immunogenicity.
Used in Diagnostic Imaging:
In diagnostic imaging, AMINO-PEG12-T-BUTYL ESTER is used to create PEGylated contrast agents. The PEGylation process can enhance the stability and circulation time of these agents, leading to improved imaging resolution and reduced side effects.
Used in Cosmetics and Personal Care:
In the cosmetics and personal care industry, AMINO-PEG12-T-BUTYL ESTER is used to improve the solubility and biocompatibility of various active ingredients. PEGylation can also provide controlled release properties, enhancing the efficacy and safety of cosmetic products.

Upstream product

• 581065-94-3 tert-butyl 3-[2-(2-{2-[2-(toluene-4-sulfonyloxy)-ethoxy]ethoxy}ethoxy)ethoxy]propionate 
• 870487-48-2 tert-butyl 1-(methanesulfonyloxy)-3,6,9,12-tetraoxapentadecan-15-oate 
• 217817-01-1 tert-butyl 3-[2-[2-[2-(4-methylphenyl)sulfonyloxyethoxy]ethoxy]ethoxy]propanoate 
• 1349193-22-1 8-dibenzylamino-3,6-dioxaoctan-1-ol 
• 252881-73-5 tert-Butyl 3-(2-(2-(2-azidoethoxyl)ethoxy)ethoxy)propanoate 
• 1663-39-4 tert-Butyl acrylate 
• 1271728-79-0 tert-butyl 3-(2-(2-azidoethoxy)ethoxy)propanoate 
• 2615-15-8 pentaethylene glycol 
• 406213-76-1 tert-butyl 1-azido-3,6,9,12,15,18-hexaoxahenicosan-21-oate 
• 361189-64-2 tert-butyl 1-hydroxy-3,6,9,12,15,18-hexaoxahenicosan-21-oate 
• 1024602-74-1 tert-butyl 3-(2-{2-[2-(methanesulphonyloxy)ethoxy]ethoxy}ethoxy)propanoate 
• 112-27-6 2,2'-[1,2-ethanediylbis(oxy)]bisethanol 
• 186020-66-6 3-{2-[2-(2-hydroxy-ethoxy)-ethoxy]-ethoxy}-propionic acid tert-butyl ester 
• 581066-04-8 tert-butyl 1-azido-3,6,9,12-tetraoxapentadecan-15-oate 

Downstream Products

• 663921-15-1 3-[2-(2-{2-[2-(2-aminoethoxy)ethoxy]ethoxy}ethoxy)ethoxy]propanoic acid 
• 867062-95-1 12-{N-[(9H-fluoren-9-yl)methoxycarbonyl]amido}-4,7,10-trioxadodecanoic acid 
• 1407510-87-5 tert-butyl(1-(3-(((3S,7S,11S)-7,11-bis(2,3-dihydroxybenzamido)-2,6,10-trioxo-1,5,9-trioxacyclododecan-3-yl)carbamoyl)-4,5-dihydroxyphenyl)-1-oxo-5,8,11-trioxa-2-azatridecan-13-yl)carbamate 
• 1609108-72-6 pentafluorophenyl 1-bromo-2-oxo-6,9,12,15,18,21-hexaoxa-3-azatetracosan-24-oate 
• 1609108-75-9 N-(24-bromo-23-oxo-4,7,10,13,16,19-hexaoxa-22-azatetracosan-1-oyl)-L-valyl-N-[2-(3-{[trans-4-({[(3R,5S,7R,8R)-8-hydroxy-7-{(1E,3E)-5-[(2S,3S,5R,6R)-5-{[(2Z,4S)-4-hydroxypent-2-enoyl]amino}-3,6-dimethyltetrahydro-2H-pyran-2-yl]-3-methylpenta-1,3-dien-1-yl}-1,6-dioxaspiro[2.5]oct-5-yl]acetyl}amino)cyclohexyl]oxy}-3-oxopropyl)phenyl]-L-alaninamide 

Relevant academic research and scientific papers

Probing the Anticancer Mechanism of (-)-Ainsliatrimer A through Diverted Total Synthesis and Bioorthogonal Ligation

Herein, we report an efficient approach for exploring the novel anticancer mechanism of (-)-ainsliatrimer A, a structurally complex and unique trimeric sesquiterpenoid, through a combined strategy of diverted total synthesis (DTS) and bioorthogonal ligation (TQ ligation), which allowed us to visualize the subcellular localization of this natural product in live cells. Further biochemical studies facilitated by pretarget imaging revealed that PPARγ, a nucleus receptor, was a functional cellular target of ainsliatrimer A. We also confirmed that the anticancer activity of ainsliatrimer A was caused by the activation of PPARγ.

CONJUGATES OF A CELL-BINDING MOLECULE WITH CAMPTOTHECIN ANALOGS

Provided are conjugates of camptothecin analogs with a cell-binding molecule of formula (I), wherein R1, R2, R3, R4, R5, X, L, n, m, T and ----- are defined herein. It also provides methods of making the conjugates of camptothecin analogs to a cell-binding agent, as well as methods of using the conjugates in targeted treatment of cancer, infection, and immunological disorders.

TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES RELATED TO EED, EZH2, OR PRC2, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound represented by formula 1, according to the present invention is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient.

CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES

A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.

CONJUGATION LINKERS CONTAINING 2,3-DIAMINOSUCCINYL GROUP

Provided is a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (adual-linker) containing a 2, 3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

A CONJUGATE OF AN AMANITA TOXIN WITH BRANCHED LINKERS

Provided herein is the conjugation of an amanita toxin compound to a cell-binding molecule with branched linkers for having better targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of an amanita molecule to a cell-binding ligand, as well as methods of using the conjugate in targets treatment of cancer, infection and autoimmune disease.

A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS

Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.

A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS

The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.

Optimization of IEDDA bioorthogonal system: Efficient process to improve trans-cyclooctene/tetrazine interaction

The antibody pretargeting approach for radioimmunotherapy (RIT) using inverse electron demand Diels-Alder cycloaddition (IEDDA) constitutes an emerging theranostic approach for solid cancers. However, IEDDA pretargeting has not reached clinical trial. The major limitation of the IEDDA strategy depends largely on trans-cyclooctene (TCO) stability. Indeed, TCO may isomerize into the more stable but unreactive cis-cyclooctene (CCO), leading to a drastic decrease of IEDDA efficiency. We have thus developed both efficient and reproducible synthetic pathways and analytical follow up for (PEGylated) TCO derivatives, providing high TCO isomeric purity for antibody modification. We have set up an original process to limit the isomerization of TCO to CCO before the mAbs’ functionalization to allow high TCO/tetrazine cycloaddition.

Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof

Disclosed are an antibody drug conjugate IB, which uses ether linkages for connection, and improves the water solubility, stability and cytotoxicity in vivo and in intro, and an intermediate, a pharmaceutical composition, and uses of the antibody drug conjugate. The antibody drug conjugate has simple synthetic steps and a high yield.