| Identification | Back 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 Properties | Back 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 | [InChI]
1S/C14H11ClN6O3/c1-8-6-13(20-19-8)17-12-7-11(15)16-14(18-12)24-10-4-2-9(3-5-10)21(22)23/h2-7H,1H3,(H2,16,17,18,19,20) | [InChIKey]
CEUMAXLRGBKFQP-UHFFFAOYSA-N | [SMILES]
Clc1nc(nc(c1)Nc3[nH]nc(c3)C)Oc2ccc(cc2)[N+](=O)[O-] |
| Hazard Information | Back 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. | [IC 50]
Vps34: 19 nM (IC50) | [storage]
Store at +4°C |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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