An inhibitor of mTORC1 and mTORC2
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Ku-0063794

Item No. 13597

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
rel-5-[2-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-benzenemethanol
CAS Number
938440-64-3
Molecular Formula
C25H31N5O4
Formula Weight
465.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 2 mg/ml
λmax
211, 229, 281, 383 nm
SMILES
OCC1=C(OC)C=CC(C2=CC=C3C(N=C(N4C[C@@H](C)O[C@@H](C)C4)N=C3N5CCOCC5)=N2)=C1
InChi Code
InChI=1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+
InChi Key
RFSMUFRPPYDYRD-CALCHBBNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $81

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    10 mg

    $152

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    50 mg

    $436

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    100 mg

    $633

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    Product Description

    Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM).1 It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks.1 Ku-0063794 inhibits cell growth by inducing G1-cell cycle arrest and autophagy, but not apoptosis, and inhibits tumor growth in a xenograft model of renal cell carcinoma (8 mg/kg for 46 days).1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. García-Martínez, J.M., Moran, J., Clarke, R.G., et al. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem. J. 421(1), 29-42 (2009).

    2. Fei, S.J., Zhang, X.C., Dong, S., et al. Targeting mTOR to overcome epidermal growth factor receptor tyrosine kinase inhibitor resistance in non-small cell lung cancer cells. PLoS One 8(7), 69104 (2013).

    3. Zhang, H., Berel, D., Wang, Y., et al. A comparison of Ku0063794, a dual mTORC1 and mTORC2 inhibitor, and temsirolimus in preclinical renal cell carcinoma models. PLoS One 8(1), 54918 (2013).