| Identification | Back 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 |
| Hazard Information | Back 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. |
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NCE Biomedical Co.,Ltd.
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| Company Name: |
SPIRO PHARMA
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www.spiropharma.com.cn |
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