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Home > Products >  N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methylurea

N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methylurea CAS NO.1144068-46-1

  • Min.Order: 5 Milligram
  • Payment Terms: T/T,Western Union,Other
  • Product Details

Keywords

  • WYE125132
  • 1144068-46-1
  • Inhibitors

Quick Details

  • ProName: N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-...
  • CasNo: 1144068-46-1
  • Molecular Formula: C27H33N7O4
  • Application: inhibitor
  • DeliveryTime: with stock
  • PackAge: 5mg,10mg,25mg,100mg
  • Port: Shanghai
  • ProductionCapacity: 10 Kilogram/Month
  • Purity: 98%
  • Storage: Store in a cool and dry place
  • Transportation: By courier
  • LimitNum: 5 Milligram

Superiority

 

 

WYE-125132 is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor.


 



Details

WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases. In vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). Besides, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size. WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover, WYE-125132 is also found to induce the dephosphorylation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus.

 

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