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WYE125132 | mTOR inhibitor

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Price:
$159.00
Catalog #:
C9125-2s
Quantity:


Product Description

WYE125132 is an orally-available, ATP-competitive, pyrazolopyrimidine-based, specific inhibitor of mTORC1 and mTORC2 with an mTOR potency of 0.19 nM and >5000-fold selectivity against the PI3K isoform family, hSMG1, and ATR enzymes. WYE125132 selectively inhibits phosphorylation of p-Akt (S473) and Akt without significantly reducing levels of T308. FACS analysis reveals that WYE125132 induces cell cycle arrest at the G1-phase, with a reduction in S-phase cells. [1]

WYE125132 induces the rapid loss of phosphorylation at Ser75. Maf1 dephosphorylation was also observed and correlated with its accumulation in the nucleus and a marked decline in the cellular levels of pre-tRNAs. [2]


Technical information:

Chemical Formula:   C27H33N7O4
CAS #:   1144068-46-1
Molecular Weight:   519.6
Purity: > 99%
Appearance:   White
Chemical Name:   Urea, 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
Solubility:   Up to 100 mM in DMSO
Synonyms:   WYN125132, WYN-132,WYN-125132

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Yu et al., Beyond Rapalog Therapy: Preclinical Pharmacology and Antitumor Activity of WYE-125132, an ATP-Competitive and Specific Inhibitor of mTORC1 and mTORC2. Cancer Res. 2010, 70, 621-631. Pubmed ID: 20068177
2. Shor et al., Requirement of the mTOR Kinase for the Regulation of Maf1 Phosphorylation and Control of RNA Polymerase III-dependent Transcription in Cancer Cells. J. Biol. Chem. 2010, 285(20), 15380-15392. Pubmed ID: 20233713

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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