A dual inhibitor of class I PI3Ks and mTOR
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Alternative(s)
21185NVP-BEZ235 (hydrochloride)
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NVP-BEZ235

Item No. 10565

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2,3-dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-α,α-dimethyl-benzeneacetonitrile
CAS Number
915019-65-7
Synonyms
  • Dactolisib
Molecular Formula
C30H23N5O
Formula Weight
469.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 1 mg/ml
λmax
266, 320 nm
SMILES
CC(C#N)(C)C(C=C1)=CC=C1N(C(N2C)=O)C3=C2C=NC4=CC=C(C5=CC(C=CC=C6)=C6N=C5)C=C43
InChi Code
InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3
InChi Key
JOGKUKXHTYWRGZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

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    100 mg

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    250 mg

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    Product Description

    NVP-BEZ235 is a dual inhibitor of class I PI3Ks (IC50s = 4, 75, 7, and 5 nM, for p110α, - β, -δ, and -γ, respectively) and mTOR (IC50 = 20 nM).1 It is selective for these enzymes over a panel of kinases (IC50s = >10 µM for all). NVP-BEZ235 (0.1 or 1 µM) inhibits proliferation of, and induces apoptosis in, MCF-7, MDA-MB-468, SK-BR-3, and MDA-MB-361 breast cancer cells.2 It reduces tumor growth in a U87MG mouse xenograft model when administered at a doses of 25, 35, or 45 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maira, S.M., Stauffer, F., Brueggen, J., et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol. Cancer Ther. 7(7), 1851-1863 (2008).

    2. Serra, V., Markman, B., Scaltriti, M., et al. NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations. Cancer Res. 68(19), 8022-8030 (2008).