Dual mTORC1/mTORC2 inhibitor
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WYE-125132

Item No. 18372

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
1144068-46-1
Synonyms
  • WYE-132
Molecular Formula
C27H33N7O4
Formula Weight
519.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 30 mg/mlEthanol: 0.4 mg/ml
λmax
203, 290 nm
SMILES
O=C(NC)NC(C=C1)=CC=C1C2=NC(N3CC4CCC(O4)C3)=C5C(N(C6CCC7(OCCO7)CC6)N=C5)=N2
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)
InChi Key
QLHHRYZMBGPBJG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $41

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    1 mg

    $69

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    5 mg

    $106

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    10 mg

    $196

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    Product Description

    WYE-125132 is an ATP-competitive inhibitor of mTOR (IC50 = 0.19 nM) that inhibits signaling through both mTORC1 and mTORC2.1 It is selective for mTOR over phosphatidylinositol 3-kinase isoforms.1 WYE-125132 is effective against mTORC1 and mTORC2 in diverse cancer models, both in vitro and in vivo.1 Oral administration of WYE-125132 alone blocks mTOR signaling and prevents tumor growth in breast, lung, renal, and glioma cancer xenografts in mice, while combination therapy with the VEGF-inhibitor bevacizumab causes complete regression of A498 renal carcinoma tumors.1 In addition to its applications in cancer, WYE-125132 has been used to delineate novel aspects of mTOR signaling.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yu, K., Shi, C., Toral-Barza, L., 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. 70(2), 621-631 (2010).

    2. Shor, B., Wu, J., Shakey, Q., et al. Requirement of the mTOR kinase for the regulation of Maf1 phosphorylation and control of RNA polymerase III-dependent transcription in cancer cells. The Journal of Biological Chemisty 285(20), 15380-15392 (2010).