Synonyms: 6-Chloro-N-(5-methyl-1H-pyrazol-3-yl)-2-(4-nitrophenoxy)-4-pyrimidinamine; 6-Chloro-N-(5-methyl-1H-pyrazol-3-yl)-2-(4-nitrophenoxy)pyrimidin-4-amine
Molecular Formula: C14H11ClN6O3
Molecular Weight: 346.73
Linear Structural Formula: C14H11ClN6O3
MDL Number: MFCD31560472
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: Autophinib is an ATP-competitive, potent and selective PI3K type 3 lipid kinase vacuolar protein sorting 34 inhibitor (VPS34 IC50/[ATP] = 19 nM/10 muM & 51 nM/100 muM) that 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 muM). 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.