WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406366
CAS#: 1144068-46-1
Description: WYE-125132, also known as WYE-132, is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L; >5,000-fold selective versus PI3Ks). WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. Importantly, consistent with genetic ablation of mTORC2, WYE-132 targeted P-AKT(S473) and AKT function without significantly reducing the steady-state level of the PI3K/PDK1 activity biomarker P-AKT(T308), highlighting a prominent and direct regulation of AKT by mTORC2 in cancer cells.
MedKoo Cat#: 406366
Name: WYE-125132
CAS#: 1144068-46-1
Chemical Formula: C27H33N7O4
Exact Mass: 519.2594
Molecular Weight: 519.6
Elemental Analysis: C, 62.41; H, 6.40; N, 18.87; O, 12.32
WYE-125132, purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Note: the estimated shipping out time for order > 10mg may be 2 months
Synonym: WYE 125132, WYE-125132, WYE125132, WYE132, WYE 132, WYE-132
IUPAC/Chemical Name: 1-(4-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-1-(1,4-dioxaspiro[4.5]decan-8-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl)-3-methylurea
InChi Key: QLHHRYZMBGPBJG-UHFFFAOYSA-N
InChi Code: InChI=1S/C27H33N7O4/c1-28-26(35)30-18-4-2-17(3-5-18)23-31-24(33-15-20-6-7-21(16-33)38-20)22-14-29-34(25(22)32-23)19-8-10-27(11-9-19)36-12-13-37-27/h2-5,14,19-21H,6-13,15-16H2,1H3,(H2,28,30,35)
SMILES Code: O=C(NC)NC1=CC=C(C2=NC(N3CC(O4)CCC4C3)=C5C(N(C(CC6)CCC76OCCO7)N=C5)=N2)C=C1
The following data is based on the product molecular weight 519.6 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Yu K, Toral-Barza L. Biochemical and pharmacological inhibition of mTOR by rapamycin and an ATP-competitive mTOR inhibitor. Methods Mol Biol. 2012;821:15-28. doi: 10.1007/978-1-61779-430-8_2. PubMed PMID: 22125057.
2: Shor B, Wu J, Shakey Q, Toral-Barza L, Shi C, Follettie M, Yu K. 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 May 14;285(20):15380-92. doi: 10.1074/jbc.M109.071639. Epub 2010 Mar 16. PubMed PMID: 20233713; PubMed Central PMCID: PMC2865278.
3: Yu K, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, Ayral-Kaloustian S, Mansour TS, Abraham RT, Zask A, Gibbons JJ. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Res. 2010 Jan 15;70(2):621-31. doi: 10.1158/0008-5472.CAN-09-2340. Epub 2010 Jan 12. PubMed PMID: 20068177.