Autophinib Chemical Properties

Boiling point:

640.6±65.0 °C(Predicted)

Density 

1.547±0.06 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO:13.98(Max Conc. mg/mL);40.32(Max Conc. mM)

form 

A solid

pka

13.78±0.10(Predicted)

color 

Light yellow to yellow

Autophinib Usage And Synthesis

Uses

Autophinib is a potent VPS34 inhibitor (IC50 = 19 nM). Inhibits starvation- and Rapamycin-induced autophagy (IC50 values = 40 and 90 nM, respectively).

Biological Activity

Autophinib is an ATP-competitive, potent and selective PI3K type 3 lipid kinase vacuolar protein sorting 34 inhibitor (VPS34 IC50/[ATP] = 19 nM/10 μM & 51 nM/100 μM) th at shows significant inhibition against only 45 kinases among a panel of >460 with little or no potency toward mTOR, TBK1 and 12 other phosphatidylinositol kinases (=22% inhibition at 1 μM). Autophinib effectively prevents autophagy induction in MCF7 cells upon amino acid starvation or rapamycin treatment (IC50 = 40 nM and 19 nM, respectively) with similar potency as SAR405 (IC50 = 53 nM and 20 nM, respectively) and VPS34-IN1 (IC50 = 13 nM and 15 nM, respectively). Autophinib enhances MCF7 cell death under starvation condition (EC50 = 264 nM and 234 nM by cytotoxiciy and apoptosis detection, respectively) by preventing autophagy-dependent cell survival.

storage

Store at +4°C

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