RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor ( IC 50 s: 1.4 nM, 1.9 nM, 3.8 nM for RET WT , RET V804L , RET V804M , respectively). RET-IN-31 inhibits hERG and Cytochrome P450 ( IC 50 s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2 , CYP2C9 , CYP2C19 , CYP2D6 , CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers.
Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > Membrane Transporter/Ion Channel | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Cancer | Products > Signaling Pathways > RET | Products > Signaling Pathways > Potassium Channel | Products > Signaling Pathways > Cytochrome P450
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