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Apeloa
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DS Technology Platforms
Flow Chemistry Synthetic Biology & Biocatalysis Highly Potent Compound Peptide TPD/PROTAC Oligonucleotide Synthesis Crystallization & Particle Engineering Preparation & Separation
TPD/PROTAC Platform
Apeloa TPD/PROTAC Platform offers comprehensive services for the development of targeted protein degradation therapeutics, including PROteolysis Trgeting Chimeras (PROTACs). With over 80 PROTAC-focused scientists and two dynamic chemistry service teams located in Boston and Hengdian, the platform provides expertise throughout the entire PROTAC development process. From target validation, hit generation, lead optimization, to clinical development, Apeloa leverages its integrated parallel synthesis platform, extensive E3 ligand, linker, and POI binder intermediate libraries, and strong analytical and ADME capabilities to drive PROTAC projects forward efficiently.
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Team
Apeloa TPD/PROTAC Platform is led by a team of highly experienced scientists, including co-inventors of two approved NDAs and one Phase II IND. The team comprises 12 Ph.D. holders with a combined synthetic chemistry experience of over 100 years, and a tot
Services
● Design, synthesis, and optimization of PROTAC molecules ● Synthesis and optimization of E3 ligands, linkers, and POI binders ● Rapid construction of early screening intermediate libraries via parallel synthesis platform ● Analytical, purification, and ADME evaluation studies ● Non-GMP and GMP scale-up production services
Equipment
●400Hz/600Hz NMR (Bruker/Avance) ●LC-Q-TOF (Agilent) ●LC-MSMS (Shimadzu/Waters/Agilent) ●GC-MSMS (Agilent/Shimadzu) ●HPLC (Waters) ●XRD (Rigaku) ●ICP-MS (Perkin Elmer)
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Extensive Intermediate Library
● Over 300 E3 ligands and ligand-linker conjugates in stock ● Expedites PROTAC synthesis and screening
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Flexible E3 Ligand and Linker Combinations
● Facilitates optimization of degradation efficiency and physiochemical properties
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Efficient Parallel Synthesis Platform
Rapid construction of intermediate libraries for early screening
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Expertise in E3 Ligand Scale-up
● Optimized synthetic routes for key clinical PROTAC ligands (e.g., Kymera CRBN, ARV-471, ARV-110) ● Improved yields, reduced costs, and addressed challenges like epimerization
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Retrosynthetic Approach for PROTAC Synthesis
● Avoids epimerization and purification challenges ● Utilizes easy-to-purify fragments and conjugate intermediates
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