915019-65-7 Dactolisib AKSci X7430
 
 
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  X7430    
Dactolisib, 98% (HPLC)
 
BEZ235
NVP-BEZ235
2-Methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile
IDENTITY
CAS Number:915019-65-7
MDL Number:MFCD10565944
MF:C30H23N5O
MW:469.54
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98% (HPLC)
Physical Form (at 20°C):Solid
Melting Point:287-291°C
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO
Application(s):Dual ATP-competitive PI3K and mTOR inhibitor
Form:Free Base
Research Area:Cancer

REVIEW
 2-Methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile (BEZ235) is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. In cellular settings using human tumor cell lines, this molecule is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. The cellular activity of NVP-BEZ235 translates well in in vivo models of human cancer. Thus, the compdound was well tolerated, displayed disease stasis when administered orally, and enhanced the efficacy of other anticancer agents when used in in vivo combination studies. Ex vivo pharmacokinetic/pharmacodynamic analyses of tumor tissues showed a time-dependent correlation between compound. concentration. and PI3K/Akt pathway inhibition. Collectively, the preclinical. data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties. Recent have indicate that the activated PI3K/Akt/mTOR signaling pathway induced by various anticancer drugs explains resistance, and BEZ235 can be used to resensitize various cancer cells.

REFERENCES
[1]Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K, Fabbro D, Gabriel D, Simonen M, Murphy L, Finan P, Sellers W, García-Echeverría C. 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. 2008 Jul;7(7):1851-63.
[2] Sznol, Joshua A.; Jilaveanu, Lucia B.; Kluger, Harriet M. Studies of NVP-BEZ235 in melanoma, Current Cancer Drug Targets (2013), 13(2), 165-174.
[3] Lin SF, Huang YY, Lin JD, Chou TC, Hsueh C, Wong RJ, Utility of a PI3K/mTOR inhibitor (NVP-BEZ235) for thyroid cancer therapy. PLoS One. 2012;7(10):e46726.
[4] Sznol JA, Jilaveanu LB, Kluger HM.Studies of NVP-BEZ235 in melanoma. Curr Cancer Drug Targets. 2013 Feb;13(2):165-74.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501

Current as of April 25, 2024


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