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      S80123

      Avagacestat (BMS-708163)

      MedMol 99%
      • 英文名:
      • Avagacestat (BMS-708163)
      • 別名:
      • (2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide
      • CAS號:
      • 1146699-66-2
      • 分子式:
      • C20H17ClF4N4O4S
      • 分子量:
      • 520.89
      貨號產品規格市場價(RMB)您的折扣價(RMB)庫存(上海) 北京 武漢 南京 數量計量單位 加入購物車...
      S80123-5mg 99% ¥1000.00元 ¥1000.00元 預計交期:2-3天 0 0 0 EA 加入購物車
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      • 提示:詳情請下載說明書。
      • 產品描述: Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
      • 靶點: IC50: 0.27 nM (γ-secretase, Aβ42), 0.30 nM (γ-secretase, Aβ40), 20 μM (CYP2C19), 0.84 nM (NICD)
      • 體內研究: Avagacestat (BMS-708163) significantly reduces both plasma and brain Aβ40 levels relative to control at 10 and 100 mg/kg for the entire dosing interval, demonstrates significant Aβ40 lowering for 8 h after an oral dose of 1 mg/kg, and significantly lowers CSF Aβ40 levels in rats, when measured 5 h after single oral doses ranging from 3 to 100 mg/kg. Avagacestat (BMS-708163) (10?mg/kg) monotherapy has a minor inhibitory effect on PC9/AB2 tumor growth compared with gefitinib alone. BMS-708163 monotherapy results in a slight increase in caspase 3 expression as well as a mild decrease in Ki-67 expression in vivo. In the xenograft lung cancer samples treated with Avagacestat (BMS-708163) plus gefitinib, there are a marked increase in caspase 3 expression and a reduction in Ki-67 staining
      • 參考文獻:
        1. Gillman KW, et al. Letter Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. Med Chem Lett, 2010, 1 (3), 120-124. 2. Xie M, et al. γ Secretase inhibitor BMS-708163 reverses resistance to EGFR inhibitor via the PI3K/Akt pathway in lung cancer. J Cell Biochem. 2015 Jun;116(6):1019-27. 3. Crump CJ, et al. BMS-708,163 targets presenilin and lacks notch-sparing activity. Biochemistry. 2012 Sep 18;51(37):7209-11. 4. Borghys H, et al. A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators. J Alzheimers Dis. 2012;28(4):809-22. 5. Vladimir Coric, et al. Safety and tolerability of the γ-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease. Arch Neurol. 2012 Nov;69(11):1430-40.
      • 溶解性: Soluble  in  DMSO
      • 保存條件: -20℃
      • 配置溶液濃度參考:
        1mg 5mg 10mg
        1 mM 1.92 ml 9.599 ml 19.198 ml
        5 mM 0.384 ml 1.92 ml 3.84 ml
        10 mM 0.192 ml 0.96 ml 1.92 ml
        50 mM 0.038 ml 0.192 ml 0.384 ml
      • 注意:部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。
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