NVP-BEZ235

    • 货号:MC0154
      • CasNo:
      • 915019-65-7
      • 分子式:
      • C30H23N5O
      • 纯度:
      • >98%
      • 靶点:
      • PI3K
      • IC50:
      • IC50: 4 nM (p110α), 5 nM (p110γ), 7 nM (p110δ), 75 nM (p110β), 6 nM (mTOR)[1]
      • 体外研究:
      • BEZ235 (NVP-BEZ235) potently inhibits PI3K in an ATP Competitive Manner. NVP-BEZ235 (250 nM) significantly reduced the phosphorylation levels of the mTOR activated kinase p70S6K. NVP-BEZ235 also leads to a reduction of S235/S236P-RPS6 levels with an IC50 of 6.5 nM, suggesting that NVP-BEZ235 can directly inhibit the mTOR kinase, as the kinase domain of mTOR is highly homologous to the one of class IA PI3K. The activity of NVP-BEZ235 against mTOR is confirmed using a biochemical mTOR K-LISA assay (IC50, 20.7 nM)[1]. The IC50s of NVP-BEZ235 for HCT116, DLD-1, and SW480 cell lines are 14.3±6.4, 9.0±1.5, and 12.0±1.6 nM, respectively[2].
      • 体内研究:
      • BEZ235 (NVP-BEZ235) (45 mg/kg, p.o.) treatment induces colonic tumor regression in a GEM model for sporadic PIK3CA wild-type CRC[2]. NVP-BEZ235 (45 mg/kg) is administered to MENX rats (n=2 each group) by oral gavage and animals are sacrificed 1 or 6 hours after treatment. Immunostains for P-AKT and P-S6 show considerable reduction of the two proteins, and particularly of P-S6, 6 hours after administration of NVP-BEZ235 when compares with PEG-treated rats. At 6 hours after treatment, the pituitary adenomas of NVP-BEZ235-treated rats has a proteomic profile significantly different from the tumors of placebo-treated rats[3].
      • 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: PI3K. 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: 4 nM (p110α), 5 nM (p110γ), 7 nM (p110δ), 75 nM (p110β), 6 nM (mTOR)[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:
      • 469.55
      • 产品图片