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Dactolisib Tosylate

Dactolisib Tosylate
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Purity:99.85%
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Dactolisib Tosylate

Catalog No. T14552Cas No. 1028385-32-1
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.
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Pack SizePrice/USDAvailabilityQuantity
25 mg$42In Stock
50 mg$59In Stock
1 mL x 10 mM (in DMSO)$65In Stock
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Product Introduction

Bioactivity
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.
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]
AliasBEZ235 Tosylate, NVP-BEZ 235 Tosylate
Chemical Properties
Molecular Weight641.74
FormulaC37H31N5O4S
Cas No.1028385-32-1
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: 0.1 mg/mL (insoluble)
DMSO: 30.6 mg/mL (47.7 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
50 mM0.0312 mL0.1558 mL0.3117 mL1.5583 mL
100 mM0.0156 mL0.0779 mL0.1558 mL0.7791 mL

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