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NVP-BEZ 235

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NVP-BEZ 235 Basic information

Product Name:
NVP-BEZ 235
Synonyms:
  • 4-[2,3-Dihydro-3-Methyl-2-oxo-8-(quinolin-3-yl)-1H-iMidazo[4,5-c]quinolin-1-yl]-alpha,alpha-diMethylbenzeneacetonitrile
  • BEZ-235
  • 2-methyl-2-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)propanenitrile
  • 2-Methyl-2-[3-Methyl-2-oxo-8-(3-quinolinyl)-1-iMidazo[4,5-c]quinolinyl]propanenitrile
  • BEZ235 (NVP-BEZ235, Dactolisib)
  • 2-Methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)phenyl
  • BEZ235 NVP-BEZ235(BEZ235)
  • Dactolisib
CAS:
915019-65-7
MF:
C30H23N5O
MW:
469.55
EINECS:
1312995-182-4
Product Categories:
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Protein Kinase Inhibitors and Activators
  • api
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
Mol File:
915019-65-7.mol
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NVP-BEZ 235 Chemical Properties

Melting point:
288-289°C
Boiling point:
701.0±70.0 °C(Predicted)
Density 
1.299
storage temp. 
Refrigerator
solubility 
Soluble in DMSO (up to 1 mg/ml with warming) or in DMF (up to 10 mg/ml, dissolves slowly, requires heating to 75?C).
pka
6.41±0.20(Predicted)
form 
White powder.
color 
White or off-white
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 1 month.
CAS DataBase Reference
915019-65-7
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NVP-BEZ 235 Usage And Synthesis

Description

NVP-BEZ235 (915019-65-7) is a dual PI3K and mTOR kinase inhibitor.1?It inhibits VEGF-induced proliferation and angiogenesis.2?Reverses lapatinib resistance.3?It induces G1 arrest and reduces cyclin D1 expression in melanoma cells with negligible apoptosis.4?NVP-BEZ235 inhibits the growth of cancer cells with activating PI3K mutations.5?The ability of NVP-BEZ235 to inhibit PI3K has come into question. This study also shows it to be a potent inhibitor of PRKDC (IC50 = 29 nM), ATM (IC50 = 13 nM), and ATR (IC50 = 8 nM).6?Active in vivo.

Chemical Properties

Light Beige Solid

Uses

A dual ATP-competitive inhibitor of PI3K and mTOR. p110α, IC50=4 nM; p110β, IC50=75 nM; p110δ, IC50=7 nM; p110γ, IC50=5 nM.

Uses

Inhibitor of phosphatidylinositol 3-kinases, P13K and mTOR.

Uses

Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of 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. It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase. Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis. By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.[Cayman Chemical]

Definition

ChEBI: An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.

in vivo

BEZ235 induced tumor regression (69%) without a statistically significant effect on weight gain. Taken together, these preliminary in vivo efficacy findings suggest that BEZ235 blocks disease progression when administered orally alone and enhances efficacy when combined with other anticancer drugs.

References

1) Maira et al. (2008), 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 1851 2) Schnell et al. (2008), 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 6598 3) Eichhorn et al. (2008), Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/Phosphatidylinositol 3-kinase inhibitor NVP-BEZ235; Cancer Res., 68 9221 4) Marone et al. (2009), Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors; Mol. Cancer Res., 7 601 5) Serra et al. (2008), NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations; Cancer Res., 68 8022 6) Reinecke?et al. (2019),?Chemoproteomic selectivity profiling of PIKK and PI3K kinase inhibitors; ACS Chem.Biol., 14?655

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