BEZ235 (Tosylate) manufacturers
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| | 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 | | EINECS: | | | Product Categories: | | | 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 | | in vivo | Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, Dactolisib (BEZ235) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM[1]. | | IC 50 | p110α: 4 nM (IC50); p110α-H1047R: 4.6 nM (IC50); p110α-E545K: 5.7 nM (IC50); p110γ: 5 nM (IC50); p110δ: 7 nM (IC50); p110β: 75 nM (IC50); mTOR: 20.7 nM (IC50); mTORC1; mTORC2; Autophagy | | 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. |
| | BEZ235 (Tosylate) Preparation Products And Raw materials |
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