[2-(4-chlorophenyl)quinolin-4-yl]-(2-piperidyl)methanol Chemical Properties

Melting point:

198-199.5 °C

Boiling point:

551.4±50.0 °C(Predicted)

Density 

1.244±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 10 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 1 mg/ml; Ethanol: 0.25 mg/ml

form 

A crystalline solid

pka

13.22±0.20(Predicted)

Safety Information

HS Code 

2933499090

[2-(4-chlorophenyl)quinolin-4-yl]-(2-piperidyl)methanol Usage And Synthesis

Description

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). 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.

Uses

Vacquinol-1 is in the vacquinol class of quinine derivatives that stimulate death in glioblastoma cells through massive macropinocytotic vacuolization, ATP depletion and eventual cytoplasmic membrane rupture.

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