Potent inhibitor of mTOR in both mTORC1 and mTORC2
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WYE-354

Item No. 13604

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[6-[4-[(methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic acid, methyl ester
CAS Number
1062169-56-5
Molecular Formula
C24H29N7O5
Formula Weight
495.5
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
287 nm
SMILES
O=C(OC)NC1=CC=C(C2=NC(N3CCOCC3)=C4C(N(C5CCN(C(OC)=O)CC5)N=C4)=N2)C=C1
InChi Code
InChI=1S/C24H29N7O5/c1-34-23(32)26-17-5-3-16(4-6-17)20-27-21(29-11-13-36-14-12-29)19-15-25-31(22(19)28-20)18-7-9-30(10-8-18)24(33)35-2/h3-6,15,18H,7-14H2,1-2H3,(H,26,32)
InChi Key
IMXHGCRIEAKIBU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.1,2 It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases.3 WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yu, K., Toral-Barza, L., Shi, C., et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 69(15), 6232-6240 (2009).

    2. Zhao, Y., Wieman, H.L., Jacobs, S.R., et al. Mechanisms and methods in glucose metabolism and cell death. Methods Enzymol. 442, 439-457 (2008).

    3. Zask, A., Verheijen, J.C., Curran, K., et al. ATP-competitive inhibitors of the mammalian target of rapamycin: Design and synthesis of highly potent selective pyrazolopyrimidines. J. Med. Chem. 52(16), 5013-5016 (2009).