Description
BEZ235 (NVP-BEZ235) can inhibit Thr308-P-Akt, Ser473-P-Akt and mTOR with IC50 of 29 nM, 8 nM and 6.5 nM.
Storage
2 years at -20centigrade Powder
Targets
Thr308-P-Akt, Ser473-P-Akt, mTOR
Molecular Formula
C30H23N5O
Chemical Name
2-methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile
Solubility
DMSO 1 mg/mL Water
In vitro
NVP-BEZ235 is an ATP competitor that potently and reversibly reduces the kinase activity of both p110 and mTOR. NVP-BEZ235 inhibits several PI3K pathway effectors, among them the serine/threonine-specific protein kinase Akt, the ribosomal protein S6, and the eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and induces nuclear translocation of forkhead transcription factor FKHRL1 (FOXO3a). The reported IC 50 s for Thr308-P-Akt and Ser473-P-Akt are 29 and 8 nmol/L, respectively, and 6.5 nmol/L for mTOR.
In vivo
The antitumor activity of NVP-BEZ235 was also evaluated in vivo using a xenograft model of BT474-derived cells overexpressing either the p110- a H1047R oncogenic mutation or an empty vector (mock control). NVP-BEZ235 significantly reduced tumor growth of both H1047R and empty vector control xenografts.
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