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HIT218695363
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HIT218695363
  • HIT ID:HIT218695363
  • Cas No:108687-08-7
  • Common Name:ART838
  • alias:ART-838, ART 838
  • IUPAC:3,5-diethyl 4-{2-[(1E)-3-(tert-butoxy)-3-oxoprop-1-en-1-yl]phenyl}-2-[(dimethylamino)methyl]-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
    IUPAC:3,5-diethyl 4-{2-[(1E)-3-(tert-butoxy)-3-oxoprop-1-en-1-yl]phenyl}-2-[(dimethylamino)methyl]-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
  • InChIKey:DKLVJXTUCNPMDC-FOCLMDBBSA-N
  • Molecular Formula:C28H38N2O6
  • Molecular Weight:498.62
  • Hydrogen Bond Donor (HBD):
  • Hydrogen Bond Acceptor (HBA):
  • LogP:
  • SMILES:CCOC(=O)C1=C(C)NC(CN(C)C)=C(C1c1ccccc1\C=C\C(=O)OC(C)(C)C)C(=O)OCC
    SMILES:CCOC(=O)C1=C(C)NC(CN(C)C)=C(C1c1ccccc1\C=C\C(=O)OC(C)(C)C)C(=O)OCC
  • ART838 is a dimeric pimeloyl urea compound notable for its potent anti-leukemic activity and favorable pharmacological properties. In vitro, ART-838 exhibits submicromolar inhibitory concentrations against all leukemia cell lines, demonstrating anti-leukemic efficacy 88 times greater than artemether. This compound remains in the body for extended periods and works synergistically with other anti-leukemic agents and novel kinase inhibitors to suppress leukemia cell growth. In immunodeficient NOD-SCID-IL2Rgnull (NSG) mice, ART-838 attains a plasma half-life longer than that of artemether, sustaining effective anti-leukemic concentrations for over 8 hours. Intermittent ART-838 treatment notably inhibited the growth of acute leukemia xenografts and primary grafts in NSG mice, surpassing the efficacy of artemether.
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