Knowledge Library
Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors
The KRAS G12D mutation subtype is present in over 40% of pancreatic ductal adenocarcinomas (PDAC), making this an important drug target. WuXi AppTec scientists recently contributed to a research article in ACS Med. Chem. Letters describing the optimization of a series of potent and selective KRAS G12D inhibitors through a structure-based drug design approach. The …Read More >
Anti-Tumor Nucleic Acid Drug Discovery Platform
Successful application of nucleic acid therapeutics faces many challenges, including delivery efficiency and off-target effects. To address these challenges, WuXi AppTec offers a full suite of nucleic acid-related services, including target validation, in vitro screening and cell-based functional assays, drug exposure analysis, biodistribution evaluation, PK/PD/efficacy testing, and safety assessment. Leverage our comprehensive platform to accelerate …Read More >
Enhertu-Induced Resistant Tumor Models
Antibody‒drug conjugates (ADCs), which combine the advantages of monoclonal antibodies with precise targeting and payloads, show great potential as cancer therapies. However, primary and secondary resistance is frequently observed, and development of next generation ADCs necessitates the establishment of resistant tumor models. WuXi AppTec offers validated, Enhertu-induced resistant tumor models to support project teams focused …Read More >
Oncology Cell Panel Screening Platform
Screen your compounds across our comprehensive cell screening panel of over 600 authenticated, validated human cancer cell lines covering 50 cancer types. We provide single agent and combination compound screening for potency and synergy, and bioinformatics analysis for mechanistic studies and biomarker discovery related to drug responses. We also offer an extensive KRAS mutant cell …Read More >
Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist
The metabotropic glutamate receptor mGluR7 is widely expressed throughout the CNS and has been implicated in numerous CNS disorders. WuXi AppTec scientists recently contributed to a study which led to the identification, optimization, and characterization of a highly potent, novel mGluR7 allosteric agonist, designated CVN636. The authors show that CVN636 has high selectivity toward mGluR7, …Read More >
Atopic Dermatitis Models
Atopic dermatitis (AD) is the most common, chronic inflammatory skin disease. To support drug discovery research in this area, WuXi AppTec offers a broad platform of validated, in vivo AD models. Our panel includes DNCB, DNFB, and MC903-induced AD models. Study readouts include histopathology scoring and measurements of serum IgE levels, transepidermal water loss, and …Read More >
Metastasis-Related In Vitro Assays and Xenograft Models
Cell migration, invasion, and adhesion are pivotal steps in cancer metastasis. To support research in this field, WuXi AppTec offers in vitro transwell migration and invasion assays using multiple cell types for assessing cell migratory behavior. In addition, our in vivo metastasis panel includes a broad range of brain, bone, and liver xenograft models covering …Read More >
Jurkat Reporter Cell Lines for Immunotherapy Drug Screening
WuXi AppTec offers Jurkat reporter cell lines for immunotherapy drug screening. Our platform includes CD8+, TCR knockout and CD16-expressing Jurkat-NFAT-Luc reporter cell lines, and validated assays (using co-cultures of Raji or A375 tumor cells) to evaluate the activity of CARs, TCRs, and bispecific antibodies. Leverage our portfolio of reporter cell lines to accelerate your research! …Read More >
Discovery of Novel GST Inhibitors Identified from a DNA-Encoded Library
WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DEL selection against a privileged scaffold to identify a compound with potent inhibition against SjGST and GSTM2. SAR studies, coupled with X-ray crystallography and structural analysis, revealed that …Read More >