PZ0321

WYE-125132

≥97% (HPLC)

• Synonym(s): 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, WYE-132
• Empirical Formula (Hill Notation): C₂₇H₃₃N₇O₄
• CAS Number: 1144068-46-1
• Molecular Weight: 519.60
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 20 mg/mL, clear
• storage temp.: −20°C
• SMILES string: N6(CC7OC(C6)CC7)c1nc(nc3[n](ncc31)C4CCC5(OCCO5)CC4)c2ccc(cc2)NC(=O)NC
• 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)
• InChI key: QLHHRYZMBGPBJG-UHFFFAOYSA-N

Description

Biochem/physiol Actions

In ovarian cancer cells, WYE-132 might prevent the activity of sphingosine kinase-1 (SphK1), leading to pro-apoptotic ceramide production.[1]

WYE-125132 (WYE-132) is a highly potent, ATP-competitive, and specific inhibitor of mTOR with an IC₅₀ value of 0.19 nM. Unlike rapamycin, which ihibits mTOR through allosteric binding to mTOR complex 1 (mTORC1) only, WYE-132 inhibits both mTORC1 and mTORC2. WYE-125132 is >5000-fold selective for mTOR vs. phosphoinositide 3-kinase (PI3K). WYE-132 induced apoptosis in a variety of cancer lines including LNCap prostate cells and H1975 lung cancer cells. WYE-132 also inhibited ovarian cancer cell growth.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3