Tos-PEG4-t-butyl Ester: Enabling the Synthesis of Promising PROTACs like BI-3663
The development of Proteolysis Targeting Chimeras (PROTACs) has opened new avenues for treating diseases, offering a mechanism to eliminate disease-causing proteins rather than just inhibiting them. The successful synthesis of these complex molecules relies heavily on the availability and quality of specialized chemical intermediates, with Tos-PEG4-t-butyl ester being a prime example.
Tos-PEG4-t-butyl ester (CAS: 217817-01-1) is a PEG-based linker widely employed in PROTAC research. Its specific chemical structure, featuring a PEG4 chain, a tosyl group, and a tert-butyl ester, makes it an ideal component for constructing heterobifunctional PROTAC molecules. The PEG chain contributes to solubility and flexibility, crucial for forming the necessary ternary complex for protein degradation. The tosyl group serves as a reactive moiety for conjugation, while the tert-butyl ester offers protection for the carboxyl group.
One of the most significant applications of Tos-PEG4-t-butyl ester is in the synthesis of BI-3663. BI-3663 is a notable example of a highly selective PTK2/FAK PROTAC. This compound leverages the capabilities of Tos-PEG4-t-butyl ester to link a target protein ligand with an E3 ligase ligand, resulting in the targeted degradation of PTK2. BI-3663 has demonstrated impressive efficacy, achieving a PTK2 degradation IC50 of 18 nM. This success underscores the critical role of Tos-PEG4-t-butyl ester in enabling the creation of potent and specific PROTACs.
For researchers and chemical synthesis providers, securing high-purity Tos-PEG4-t-butyl ester is essential for reproducible and successful PROTAC development. NINGBO INNO PHARMCHEM CO.,LTD. supplies this vital intermediate, supporting the scientific community in its endeavors to create novel therapeutic agents. The availability of such intermediates facilitates the exploration of new PROTAC designs and the optimization of existing ones.
As the field of targeted protein degradation continues its rapid advancement, molecules like BI-3663, made possible by advanced linkers such as Tos-PEG4-t-butyl ester, represent the future of medicine. The ability to precisely design and synthesize these complex molecules is key to unlocking their full therapeutic potential.
Tos-PEG4-t-butyl ester (CAS: 217817-01-1) is a PEG-based linker widely employed in PROTAC research. Its specific chemical structure, featuring a PEG4 chain, a tosyl group, and a tert-butyl ester, makes it an ideal component for constructing heterobifunctional PROTAC molecules. The PEG chain contributes to solubility and flexibility, crucial for forming the necessary ternary complex for protein degradation. The tosyl group serves as a reactive moiety for conjugation, while the tert-butyl ester offers protection for the carboxyl group.
One of the most significant applications of Tos-PEG4-t-butyl ester is in the synthesis of BI-3663. BI-3663 is a notable example of a highly selective PTK2/FAK PROTAC. This compound leverages the capabilities of Tos-PEG4-t-butyl ester to link a target protein ligand with an E3 ligase ligand, resulting in the targeted degradation of PTK2. BI-3663 has demonstrated impressive efficacy, achieving a PTK2 degradation IC50 of 18 nM. This success underscores the critical role of Tos-PEG4-t-butyl ester in enabling the creation of potent and specific PROTACs.
For researchers and chemical synthesis providers, securing high-purity Tos-PEG4-t-butyl ester is essential for reproducible and successful PROTAC development. NINGBO INNO PHARMCHEM CO.,LTD. supplies this vital intermediate, supporting the scientific community in its endeavors to create novel therapeutic agents. The availability of such intermediates facilitates the exploration of new PROTAC designs and the optimization of existing ones.
As the field of targeted protein degradation continues its rapid advancement, molecules like BI-3663, made possible by advanced linkers such as Tos-PEG4-t-butyl ester, represent the future of medicine. The ability to precisely design and synthesize these complex molecules is key to unlocking their full therapeutic potential.
Perspectives & Insights
Molecule Vision 7
“This compound leverages the capabilities of Tos-PEG4-t-butyl ester to link a target protein ligand with an E3 ligase ligand, resulting in the targeted degradation of PTK2.”
Alpha Origin 24
“BI-3663 has demonstrated impressive efficacy, achieving a PTK2 degradation IC50 of 18 nM.”
Future Analyst X
“This success underscores the critical role of Tos-PEG4-t-butyl ester in enabling the creation of potent and specific PROTACs.”