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ChemicalBook--->CAS DataBase List--->1644443-47-9

1644443-47-9

1644443-47-9 Structure

1644443-47-9 Structure
IdentificationBack Directory
[Name]

Autophinib
[CAS]

1644443-47-9
[Synonyms]

CS-2834
Autophinib
6-Chloro-N-(5-methyl-1H-pyrazol-3-yl)-2-(4-nitrophenoxy)-pyrimidinamine
6-CHLORO-N-(5-METHYL-1H-PYRAZOL-3-YL)-2-(4-NITROPHENOXY)PYRIMIDIN-4-AMINE
4-Pyrimidinamine, 6-chloro-N-(5-methyl-1H-pyrazol-3-yl)-2-(4-nitrophenoxy)-
[Molecular Formula]

C14H11ClN6O3
[MDL Number]

MFCD31560472
[MOL File]

1644443-47-9.mol
[Molecular Weight]

346.73
Chemical PropertiesBack Directory
[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
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack Directory
[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-competitivepotent 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 mTORTBK1 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 nMrespectively) with similar potency as SAR405 (IC50 = 53 nM and 20 nMrespectively) and VPS34-IN1 (IC50 = 13 nM and 15 nMrespectively). Autophinib enhances MCF7 cell death under starvation condition (EC50 = 264 nM and 234 nM by cytotoxiciy and apoptosis detectionrespectively) by preventing autophagy-dependent cell survival.
[storage]

Store at +4°C
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