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ChemicalBook--->CAS DataBase List--->1028385-32-1

1028385-32-1

1028385-32-1 Structure

1028385-32-1 Structure
IdentificationBack Directory
[Name]

BEZ235 (Tosylate)
[CAS]

1028385-32-1
[Synonyms]

BEZ235 (Tosylate)
Dactolisib Tosylate
NVP-BEZ 235 Tosylate
DACTOLISIB TOSYLATE (BEZ235 TOSYLATE)
NVP-BEZ 235 Tosylate (BEZ235 Tosylate)
4-methylbenzenesulfonic acid,2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile
2-Methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)- phenyl]propionitrile p-toluenesulfonate salt
4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-alpha,alpha-dimethylbenzeneacetonitrile 4-methylbenzenesulfonate
[Molecular Formula]

C37H31N5O4S
[MDL Number]

MFCD22124509
[MOL File]

1028385-32-1.mol
[Molecular Weight]

641.738
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Powder
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[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.
[Biological Activity]

bez235 is an imidazoquinoline derivative inhibiting both pi3k and mtor kinases with low nanomolar ic50s. it was well tolerated in preclinical animal studies as well as in
[References]

1. maira sm, 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 2008; 7: 1851-1863.2. markman b, tabernero j, krop i et al. phase i safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mtor inhibitor bgt226 in patients with advanced solid tumors. ann oncol 2012; 23: 2399-2408.3. schnell cr, stauffer f, allegrini pr 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 2008; 68: 6598-6607.4. mukherjee b, tomimatsu n, amancherla k et al. the dual pi3k/mtor inhibitor nvp-bez235 is a potent inhibitor of atm- and dna-pkcs-mediated dna damage responses. neoplasia 2012; 14: 34-43.5. 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 2008; 68: 8022-8030.
Spectrum DetailBack Directory
[Spectrum Detail]

BEZ235 (Tosylate)(1028385-32-1)1HNMR
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