Dactolisib Tosylate (BEZ235 Tosylate) is an inhibitor of dual PI3K and mTOR kinase(IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively). Dactolisib Tosylate also inhibits mTORC1 and mTORC2.

Dactolisib (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 PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively, and it is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of Dactolisib (BEZ235), with an average GI50 of 10 to 12 nM[1]. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest.

Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally. It 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].

1028385-32-1

C37H31N5O4S

641.74

NVP-BEZ 235 Tosylate;BEZ235 Tosylate

DMSO:34 mg/mL (52.98 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years