MTHFD1/2-IN-1

Overview

MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC 50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2 , respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia ( AML ) in mouse models.

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Blood Disease | Products > Disease Areas > Acute Myeloid Leukemia | 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 > Methylenetetrahydrofolate Dehydrogenase (MTHFD)

Product Information

• Catalog No.: HY-182356
• CAS No.: 3125953-25-2
• Molecular Formula: C30H36F3N5O6S
• Molecular Weight: 651.70
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source