Dactolisib Tosylate

SKU: orb1707567

Description

Dactolisib Tosylate

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1028385-32-1
• MW: 641.74
• Purity: 99.91%
• Formula: C₃₇H₃₁N₅O₄S
• SMILES: Cc1ccc(cc1)S(O)(=O)=O.Cn1c2cnc3ccc(cc3c2n(-c2ccc(cc2)C(C)(C)C#N)c1=O)-c1cnc2ccccc2c1
• Target: Autophagy,mTOR,PI3K
• Solubility: H2O:0.1 mg/mL (0.16 mM);DMSO:30.6 mg/mL (47.68 mM);10% DMSO+90% Corn Oil:1 mg/mL (1.56 mM)

Bioactivity

• Target IC50:
  p110α-H1047R:4.6 nM|p110β:75 nM|p110δ:7 nM|p110α:4 nM|p110γ:5 nM|p110α-E545K:5.7 nM|mTOR:20.7 nM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dactolisib Tosylate, BEZ 235 Tosylate, BEZ235 Tosylate, BEZ-235 Tosylate, Autophagy, mTORC1, mTORC2, mTOR, NVP-BEZ 235 Tosylate, NVP-BEZ235 Tosylate, NVP-BEZ-235 Tosylate, p110β, p110δ, p110γ, p110α, p110α-H1047R, p110α-E545K, PI3K

Compound Identifiers

PubChem CID

49803145