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21(4):271-281
in the cytosol
InChi: InChI=1S/C19H20N2O7/c22-14-9-8-12(17(25)20-14)21-18(26)11-5-4-6-13(16(11)19(21)27)28-10-3-1-2-7-15(23)24/h4-6
Formula: C16H21N3O2S
InChiKey: UMKPISXYUQWXJJ-XWOHEVPJSA-N
BEZ235 Tosylate 2357 (Givinostat) 21(4):271-281Dactolisib tosylate is also known as NVP BEZ 235 Tosylate. NVP 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. The IC50s for PI3K, , , are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KE545K or PI3KH1047R with IC50s of 5. 7 and 4. 6 nM, respectively. In human tumor cell lines, it is able to effectively and