Knowledge Library

Large-scale synthesis of a Notum inhibitor employing a modified Sakai reaction as the key step

WuXi AppTec scientists recently contributed to a research article in the Royal Society of Chemistry describing the large-scale synthesis of a potent and selective inhibitor of Notum carboxylesterase (an enzyme that suppresses Wnt signaling pathways).  By employing a modified Sakai reaction as the key step, a one-pot synthesis of this Notum inhibitor was developed, enabling …Read More >

Resource Type: Latest Science Publication
Resource Topic: Cardiovascular & Metabolic Diseases Discovery Chemistry Liver Diseases Oncology Respiratory Diseases Small Molecules

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Fluoroalkane modified cationic polymers for personalized mRNA cancer vaccines

Delivery carriers are a critical component in the development of mRNA vaccines. Here, we describe the synthesis of a cationic polymer as a carrier for mRNA cancer vaccine delivery. In vivo results show that this polymer-based mRNA vaccine significantly delays tumor growth after vaccination of mice. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9743697/  

Resource Type: Latest Science Publication
Resource Topic: Oncology Tumor Models

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KRAS-related Genetically Engineered Cell Lines and In Vivo Models

KRAS mutant proteins that drive cancer development are highly similar in sequence and structure. Direct inhibitors are most likely to bind to the catalytic domain of KRAS. However, recent studies have found that KRAS mutants can also be targeted by heterogeneous sites, to develop covalent inhibitors of KRAS mutants. The discovery of inhibitors that selectively …Read More >

Resource Type: Latest Science Presentation
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Cells and Protein Science Hit Finding Hit-to-Lead Lead Optimization Oncology Small Molecules Tumor Models

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WuXi Biology Fact Sheet

Expertise in all major disease areas and all major target classes, enabling discovery for all therapeutic modalities World class antiviral platform with an unequalled service capability and capacity in HBV and other viral diseases A global leader in DNA Encoded Library (DEL) screening, with innovative business models CAP-certified pathology and FACS capabilities supporting clinical biomarker …Read More >

Resource Type: Brochure Latest Science
Resource Topic: DRUG DISCOVERY AND INNOVATION TECHNOLOGY PLATFORMS THERAPEUTIC AREAS

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Targeted Protein Degradation

WuXi AppTec utilizes state-of-the-art techniques to support drug discovery teams focused on targeted protein degradation. Our services include a broad range of ligand-finding methods, such as DEL, fragment screening, ASMS, and virtual screening. We provide custom linker design and complex synthesis for new linkers and E3 ligase ligands. To support lead optimization efforts, our platform …Read More >

Resource Type: Brochure Latest Science
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Mass Spectrometry-based Assays Oncology Small Molecules Structural Biology Targeted Protein Degradation

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In Vitro Imaging Services

Offering a comprehensive platform of in vitro imaging-based assays to screen compounds for cancer, inflammation, and autoimmune diseases. Our services include: Imaging assays for cell proliferation and apoptosis Imaging assays for cell cycle analysis Cell-based functional assays, including: Antibody internalization Live-cell immunocytochemistry Cellular movement and morphology monitoring Assays for 3D cell models, including: Spheroid growth …Read More >

Resource Type: Latest Science Presentation
Resource Topic: Biomarkers Cell-based Assays Hit-to-Lead Lead Optimization Oncology Phenotypic Assays Target Identification and Validation

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CDK4/6 Inhibitor Resistant Breast Cancer Models

Leverage our extensive panel of CDK4/6 inhibitor resistant breast cancer models, including:  In vitro induced Palbociclib resistant MCF-7 cell line In vivo induced Palbociclib resistant MCF-7 model In vivo induced Abemaciclib resistant MCF-7 model In vivo induced Ribociclib resistant MCF-7 model View additional drug-resistant models in our platform

Resource Type: Latest Science Presentation
Resource Topic: Cell-based Assays Oncology Target-Specific Assays Tumor Models

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Ligand Finding and Chemistry Workflows for Targeted Protein Degradation

This webinar will focus on aspects related to PROTAC discovery and chemistry workflows, such as ligand finding strategies, synthesis optimization, and linker design. Successful development of bifunctional molecules requires a deep understanding of multiple processes, including biophysical events which dictate induced proximity and how technologies such as DNA-encoded libraries (DEL) can be leveraged to identify …Read More >

Resource Type: Webinar
Resource Topic: Autoimmune and Inflammatory Diseases Biophysical Assays Cardiovascular & Metabolic Diseases Central Nervous System & Pain Discovery Chemistry DNA-Encoded Library (DEL) Hit Finding Hit-to-Lead Lead Optimization Oncology Small Molecules Structural Biology Target-Specific Assays Targeted Protein Degradation

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Biological Characterization and Development Workflows for Targeted Protein Degradation

This webinar will focus on PROTAC biology workflows, such as in vitro screening assays, in vivo testing, and optimization of DMPK properties. Topics will include the best use of biochemical assays to measure binary/ternary complex formation, cell-based assays to assess target engagement and degradation, strategies for enhancing drug delivery and formulation, and PK/PD evaluation of …Read More >

Resource Type: Webinar
Resource Topic: Autoimmune and Inflammatory Diseases Biochemical Assays Cardiovascular & Metabolic Diseases Cell-based Assays Central Nervous System & Pain Hit-to-Lead in vitro biology in vivo Pharmacology Lead Optimization Oncology Small Molecules Target Identification and Validation Target-Specific Assays Targeted Protein Degradation

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