BEZ235 (Tosylate)
BEZ235 (Tosylate) Basic information
- Product Name:
- BEZ235 (Tosylate)
- Synonyms:
-
- BEZ235 (Tosylate)
- NVP-BEZ 235 Tosylate
- 4-[2,3-Dihydro-3-methyl-2-oxo-8-(3-quinolinyl)-1H-imidazo[4,5-c]quinolin-1-yl]-alpha,alpha-dimethylbenzeneacetonitrile 4-methylbenzenesulfonate
- NVP-BEZ 235 Tosylate (BEZ235 Tosylate)
- 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-methylbenzenesulfonic acid,2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile
- Dactolisib Tosylate
- DACTOLISIB TOSYLATE (BEZ235 TOSYLATE)
- CAS:
- 1028385-32-1
- MF:
- C37H31N5O4S
- MW:
- 641.75
- Mol File:
- 1028385-32-1.mol
BEZ235 (Tosylate) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- color
- Off-white to light yellow
BEZ235 (Tosylate) Usage And Synthesis
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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