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S80123

Avagacestat (BMS-708163)

源葉(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(hào):
  • 1146699-66-2
  • 分子式:
  • C20H17ClF4N4O4S
  • 分子量:
  • 520.89
品牌貨號(hào)產(chǎn)品規(guī)格價(jià)格(RMB) 庫(kù)存(上海) 北京 武漢 南京 數(shù)量計(jì)量單位 加入購(gòu)物車(chē)...
源葉(MedMol) S80123-1mg ≥99% ¥520.00元 10 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S80123-5mg ≥99% ¥650.00元 1 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S80123-10mg ≥99% ¥849.00元 3 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S80123-50mg ≥99% ¥2980.00元 預(yù)計(jì)交期:2-3天 - - - EA 加入購(gòu)物車(chē)
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  • 提示:詳情請(qǐng)下載說(shuō)明書(shū)。
  • 產(chǎn)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(diǎn): IC50: 0.27 nM (γ-secretase, Aβ42), 0.30 nM (γ-secretase, Aβ40), 20 μM (CYP2C19), 0.84 nM (NICD);Gamma-secretase
  • 體內(nèi)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(xiàn):
    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
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