An ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2; effective in diverse cancer models

WYE-125132 – 5 mg

Brand:
Cayman
CAS:
1144068-46-1
Storage:
-20
UN-No:
Non-Hazardous - /

The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. WYE-125132 is an ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2.{29888} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms.{29888} WYE-125132 is effective against mTORC1 and mTORC2 in diverse cancer models, both in vitro and in vivo.{29888} Oral administration of WYE-125132 alone blocks mTOR signaling and prevents tumor growth in breast, lung, renal, and glioma cancer xenografts in mice, while combination therapy with the VEGF-inhibitor bevacizumab causes complete regression of A498 renal carcinoma tumors.{29888} In addition to its applications in cancer, WYE-125132 has been used to delineate novel aspects of mTOR signaling.{29887}  

 

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Description

An ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2; effective in diverse cancer models, both in vitro and in vivo, blocking mTOR signaling and preventing growth in breast, lung, renal, and glioma cancer cells and tumor xenografts in mice

Formal name: 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’-methyl-urea

Synonyms:  WYE-132

Molecular weight: 519.6

CAS: 1144068-46-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling

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