my account
Login
  Loading... Please wait...

Product Details

NVP-BEZ235 | PI 3-K and mTOR inhibitor

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).Active in vivo.

References/Citations
1) Maira et al. (2008), Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian targe 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

 

swipe
Focus Biomolecules supplier, chemical structure of NVP-BEZ235 | PI 3-K and mTOR inhibitor | CAS 915019-65-7

Catalog#  10-2153-0010

$40.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
Request Bulk Quote
CAS:
915019-65-7
Catalog Number:
10-2153
Activity:
PI 3-K and mTOR inhibitor
Chemical Name:
2-Methyl-2-{4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile
Molecular Weight:
469.55
Molecular Formula:
C30H23N5O
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).
Physical Properties:
White or off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

Connect with Focus

Click the button below to add the NVP-BEZ235 | PI 3-K and mTOR inhibitor to your wish list.