Vacquinol-<wbr/>1

Vacquinol-1

CAT N°: 16321
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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}

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