2225940-52-1

Basic information

• Product Name: 4-((14-amino-3,6,9,12-tetraoxatetradecyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
• CAS NO: 2225940-52-1
• Molecular Weight: 492.529
• Mol File: 2225940-52-1.mol
• Article Data: 10

Chemical Properties

• CAS DataBase Reference: 4-((14-amino-3,6,9,12-tetraoxatetradecyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione(CAS DataBase Reference)
• NIST Chemistry Reference: 4-((14-amino-3,6,9,12-tetraoxatetradecyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione(2225940-52-1)
• EPA Substance Registry System: 4-((14-amino-3,6,9,12-tetraoxatetradecyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione(2225940-52-1)

Safety Data

• Hazardous Substances Data: 2225940-52-1(Hazardous Substances Data)

Upstream product

• 652-39-1 3-fluorophthalic anhydride 
• 2686-86-4 3-aminopiperidine-2,6-dione hydrochloric acid salt 
• 811442-84-9 tert-butyl N-[2-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]ethyl]carbamate 
• 835616-60-9 2‐(2,6‐dioxopiperidin‐3‐yl)‐4‐fluoroisoindoline‐1,3‐dione 
• 2271036-47-4 4-((14-azido-3,6,9,12-tetraoxatetradecyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione 

Relevant articles and documents

Discovery of novel BTK PROTACs for B-Cell lymphomas

Bruton's tyrosine kinase (BTK) is a key drug target for B-cell related malignancies. Irreversible covalent BTK inhibitors have been approved for the treatment of B-cell malignancies, yet BTK C481S mutation at the covalent binding site has caused drug-resistance of BTK covalent binding inhibitors. The proteolysis targeting chimera (PROTAC) technology increases the sensitivity to drug-resistant targets compared to classic inhibitors, which provides a new strategy for mutant BTK related B-cell malignancies. ARQ531, a reversible non-covalent BTK inhibitor that inhibits wild type (WT) and mutated BTK with high selectivity, could be an ideal warhead for PROTACs targeting the mutant BTK. Herein, we designed a novel series of PROTACs using the selective non-covalent BTK inhibitor ARQ531 as warhead, with the goal of improving the degradation of both wild-type and C481S mutant BTKs, and increasing the selectivity of BTK over other kinases. This effort will provide some basis for further preclinical study of BTK PROTACs as a novel strategy for treatment of B-cell lymphomas.

TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE

This disclosure relates to bivalent compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the bivalent compounds, and to methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such bivalent compounds.

WEE1 Protein degradation agent

WEE1 Protein degradation agents are provided. , The invention provides a compound as shown V, or a pharmaceutically acceptable salt thereof, or a stereoisomer, Y-L-M thereof. WEE1 (V) Wherein M. WEE1 A WEE1 binding moiety capable of binding to WEE1 protein kinase is provided. Y Is E3 ubiquitin ligase ligand moiety, and L Is a linking group.