Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor that targets PI3K and mTOR. dactolisib Tosylate exhibits IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. dactolisib Tosylate inhibits mTORC1 and mTORC2.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | In stock | $ 42.00 | |
50 mg | In stock | $ 59.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 65.00 |
Description | Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor that targets PI3K and mTOR. dactolisib Tosylate exhibits IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. dactolisib Tosylate inhibits mTORC1 and mTORC2. |
Targets&IC50 | mTOR:20.7 nM, p110α-E545K:5.7 nM, p110α:4 nM, p110γ:5 nM, p110δ:7 nM, p110α-H1047R:4.6 nM, p110β:75 nM |
In vitro | Dactolisib (BEZ235) exhibits IC50 values of 4 nM, 75 nM, 7 nM, and 5 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Furthermore, it demonstrates significant activity against mutant forms of PI3Kα, specifically PI3KαE545K and PI3KαH1047R, with IC50 values of 5.7 nM and 4.6 nM, respectively. Treatment with increasing concentrations of Dactolisib (BEZ235) leads to a dose-dependent reduction in cell proliferation in PTEN-null cell lines PC3M and U87MG, with an average GI50 ranging from 10 to 12 nM. Notably, in human tumor cell lines, it effectively and specifically blocks the aberrant activation of the PI3K pathway, leading to G1 arrest.[1] |
In vivo | Dactolisib (BEZ235) (50 mg/kg) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM. BEZ235 is well tolerated, and displays disease stasis when administered orally. It enhances the efficacy of other anticancer agents.[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 1 year
H2O: 0.1 mg/mL (insoluble)
DMSO: 30.6 mg/mL (47.7 mM), Sonification and heating are recommended.
You can also refer to dose conversion for different animals. More
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Dactolisib Tosylate 1028385-32-1 PI3K/Akt/mTOR signaling PI3K mTOR BEZ-235 Tosylate BEZ 235 Tosylate BEZ235 Tosylate NVP-BEZ235 Tosylate NVP-BEZ 235 Tosylate NVP-BEZ-235 Tosylate inhibitor inhibit