An inhibitor of the catalytic site of mTOR

OSI-027 – 1 mg

Brand:
Cayman
CAS:
936890-98-1
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. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively).{29740,29741} It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase.{29741} OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 µM.{29740,29742,29743} OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.{29741,29739}  

 

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Description

An inhibitor of the catalytic site of mTOR, inhibiting both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively); prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 µM; effective in vivo

Formal name: trans-4-[4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]-cyclohexanecarboxylic acid

Synonyms: 

Molecular weight: 406.4

CAS: 936890-98-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy

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