Dual inhibitor of PI3K and mTOR
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Alternative(s)
10565NVP-BEZ235
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NVP-BEZ235 (hydrochloride)

Item No. 21185

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, monohydrochloride
CAS Number
2319647-83-9
Synonyms
  • Dactolisib
Molecular Formula
C30H23N5O • HCl
Formula Weight
506.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.5 mg/mlDMSO: 1 mg/mlEthanol: 0.5 mg/ml
λmax
267 nm
SMILES
CN(C1=C(N2C3=CC=C(C(C)(C)C#N)C=C3)C4=CC(C5=CC(C=CC=C6)=C6N=C5)=CC=C4N=C1)C2=O.Cl
InChi Code
InChI=1S/C30H23N5O.ClH/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;1H
InChi Key
VDZVGMJFBACERH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    10 mg

    $36

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    25 mg

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    50 mg

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    100 mg

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    Product Description

    NVP-BEZ235 is a potent dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies.1,2 It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase.1,3 Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis.4 By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.5,6

    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. Zitzmann, K., von Rüden, J., Brand, S., et al. Compensatory activation of Akt in response to mTOR and Raf inhibitors - a rationale for dual-targeted therapy approaches in neuroendocrine tumor disease. Cancer Lett. 295(1), 100-109 (2010).

    3. 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).

    4. Schnell, C.R., Stauffer, F., Allegrini, P.R., et al. Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: Implications for clinical imaging. Cancer Res. 68(16), 6598-6607 (2008).

    5. Marone, R., Erhart, D., Mertz, A.C., et al. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol. Cancer Res. 7(4), 601-613 (2009).

    6. Brachmann, S.M., Hofmann, I., Schnell, C., et al. Specific apoptosis induction by the dual PI3K/mTOR inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells. Proc. Natl. Acad. Sci. USA 106(52), 22299-22304 (2009).