Pyridine is a six-membered heterocyclic compound containing one nitrogen heteroatom. Pyridine and piperidine are the most frequently occurring heterocyclic building blocks in drug molecules. According to incomplete statistics, there are currently more than 180 drugs containing pyridine or piperidine structure that have been marketed, nearly 1/5 of the drugs approved for marketing in recent years contain these two structures.
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Pyridine is a basic heterocyclic organic compound with the chemical formula C5H5N. It is structurally related to benzene, with one methine group (=CH−) replaced by a nitrogen atom. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell.
IAG933 is a potent, selective, and first-in-class inhibitor from Novartis that directly inhibits the protein-protein interaction (PPI) between YAP/TAZ and TEAD. By blocking this PPI, IAG933 interferes with oncogenic functions downstream of the Hippo signaling pathway, particularly in mesothelioma and other tumors with NF2 loss-of-function mutations or YAP/TAZ fusions. This inhibition reduces transcriptional activity and induces cell death in cancer cells, leading to significant tumor regressions in xenograft models. Additionally, combining IAG933 preclinically with other targeted therapies (i.e., RTK, KRAS-mutant selective, and MAPK inhibitors) shows promise for improving the efficacy and durability of treatment responses. IAG933 is currently being evaluated in a Ph. I trial (NCT04857372) for solid tumors with Hippo pathway alterations. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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