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.
