NVP-BEZ235 Tosylate

    • 货号:MC1026
      • CasNo:
      • 1028385-32-1
      • 分子式:
      • C37H31N5O4S
      • 纯度:
      • >98%
      • 靶点:
      • mTOR
      • IC50:
      • IC50: 4nM (PI3Kα), 75 nM (PI3Kβ), 7 nM (PI3Kγ), 5 nM (PI3Kδ)[1]
      • 体外研究:
      • NVP-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. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of NVP-BEZ235, with an average GI50 of 10 to 12 nM[1].
      • 体内研究:
      • NVP-BEZ235 is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, NVP-BEZ235 appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM[1].
      • 简介:
      • BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.
      • 特异性:
      • Target: mTOR . Fields: BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits A
      • 来源:
      • Rabbit
      • 稀释:
      • IC50: 4nM (PI3Kα), 75 nM (PI3Kβ), 7 nM (PI3Kγ), 5 nM (PI3Kδ)[1]
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • BEZ235
      • 分子量:
      • 641.74
      • 产品图片