A dual inhibitor of PI3K and mTOR
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GNE-493

Item No. 29224

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(2-amino-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine-6-methanol
CAS Number
1033735-94-2
Molecular Formula
C17H20N6O2S
Formula Weight
372.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 16 mg/mlEthanol: 0.5 mg/ml
λmax
271 nm
SMILES
NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C=C(C(C)(O)C)S4)=N2)C=N1
InChi Code
InChI=1S/C17H20N6O2S/c1-17(2,24)12-7-11-13(26-12)15(23-3-5-25-6-4-23)22-14(21-11)10-8-19-16(18)20-9-10/h7-9,24H,3-6H2,1-2H3,(H2,18,19,20)
InChi Key
LEXMMFPAPDGYGZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    GNE-493 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 3.4, 12, 16, 16, and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively).1 It inhibits proliferation of PC3 and MCF-7.1 cells with IC50 values of 330 and 180 nM, respectively. GNE-493 (10 mg/kg per day) reduces tumor volume in PC3 and MCF-7.1 mouse xenograft models, which are PTEN negative or PI3Kα activating mutation positive, respectively. It also decreases relative levels of phosphorylated Akt, PRAS40, and S6RP in tumor tissue in the MCF-7.1 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sutherlin, D.P., Sampath, D., Berry, M., et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors. J. Med. Chem. 53(3), 1086-1097 (2010).