Vacquinol-<wbr/>1

Vacquinol-1

CAT N°: 16321
Price:

From 77.00 65.45

Vacquinols are a new class of quinine-derivatives that stimulate death in glioblastoma cells by massive macropinocytotic vacuolization, ATP depletion, and cytoplasmic membrane rupture.{26440} A key effector of vacquinols is MAPK kinase 4 (MKK4).{26440} Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.{26440} It induces ATP depletion in glioblastoma cells (IC50 = 3.14 µM at 1 day) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells.{26440} Vacquinol-1 is orally bioavailable with good brain penetrance and excellent pharmacokinetics.{26440} Oral administration of vacquinol-1 (20 mg/kg once daily for five days) substantially impairs the growth of engrafted glioblastoma cell tumors in mice and prolongs survival.{26440}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-(4-chlorophenyl)-?-2-piperidinyl-4-quinolinemethanol
  • Correlated keywords
    • 1449743-76-3 biochemical cancer signal transduction quinine derivative cell death apoptosis glioblastoma activator NSC 13316
  • Product Overview:
    Vacquinols are a new class of quinine-derivatives that stimulate death in glioblastoma cells by massive macropinocytotic vacuolization, ATP depletion, and cytoplasmic membrane rupture.{26440} A key effector of vacquinols is MAPK kinase 4 (MKK4).{26440} Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.{26440} It induces ATP depletion in glioblastoma cells (IC50 = 3.14 µM at 1 day) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells.{26440} Vacquinol-1 is orally bioavailable with good brain penetrance and excellent pharmacokinetics.{26440} Oral administration of vacquinol-1 (20 mg/kg once daily for five days) substantially impairs the growth of engrafted glioblastoma cell tumors in mice and prolongs survival.{26440}

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