Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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.
Description | 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. |
Targets&IC50 | p110α:4 nM, p110α-E545K:5.7 nM, mTOR:20.7 nM, p110γ:5 nM, p110β:75 nM, p110α-H1047R:4.6 nM, p110δ:7 nM |
In vitro | 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. |
In vivo | 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]. |
Synonyms | BEZ235 Tosylate, NVP-BEZ 235 Tosylate |
Molecular Weight | 641.74 |
Formula | C37H31N5O4S |
CAS No. | 1028385-32-1 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 34 mg/mL (52.98 mM), Need ultrasonic and warming
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Dactolisib Tosylate 1028385-32-1 PI3K/Akt/mTOR信号通路 自噬 mTOR Autophagy PI3K BEZ235 Tosylate NVP-BEZ 235 Tosylate Inhibitor inhibitor inhibit