2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Vacquinols are a new class of quinine-derivatives that stimulate death in glioblastoma cells by massive macropinocytotic vacuolization, ATP depletion, and cytoplasmic membrane rupture.A key effector of vacquinols is MAPK kinase 4 (MKK4).1 Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.It induces ATP depletion in glioblastoma cells (IC50 = 3.14 µM at 1 day) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells.Vacquinol-1 is orally bioavailable with good brain penetrance and excellent pharmacokinetics.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.
