生物活性 靶点 体外研究 体内研究 (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione 试剂级价格
ChemicalBook  CAS数据库列表  (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione

(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione

(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione,847928-32-9,结构式
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
  • CAS号:847928-32-9
  • 英文名:(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
  • 中文名:(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
  • CBNumber:CB23367548
  • 分子式:C29H30F2N4O2
  • 分子量:504.57
  • MOL File:847928-32-9.mol
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione化学性质
  • 沸点 :674.3±55.0 °C(Predicted)
  • 密度 :1.304±0.06 g/cm3(Predicted)
  • 储存条件 :2-8°C(protect from light)
  • 溶解度 :Soluble in DMSO (>20 mg/ml)
  • 酸度系数(pKa) :7.25±0.33(Predicted)
  • 形态 :solid
  • 颜色 :Off-white
  • 稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione性质、用途与生产工艺

  • 生物活性 1G244 是一种有效的 DPP8/9 抑制剂,IC50 分别为 12 nM 和 84 nM,但不抑制 DPPIV 和 DPPII。1G244 可诱导多发性骨髓瘤细胞凋亡,并具有抗骨髓瘤作用。
  • 靶点

    IC50: 12 nM (DPP8), 84 nM (DPP9)

  • 体外研究

    1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines.
    1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected.

    Cell Viability Assay

    Cell Line: Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells
    Concentration: 0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM
    Incubation Time: 72 hours
    Result: Dose-dependently decreased viable cell number of five multiple myeloma cell lines.

    Western Blot Analysis

    Cell Line: MM.1 S cells
    Concentration: 50 μM
    Incubation Time: 0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours
    Result: Decreased caspase-3 and PARP protein.
  • 体内研究

    1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model.

    Animal Model: NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells
    Dosage: 30 mg/kg
    Administration: Subcutaneous injection; once-a-week; for 3 weeks
    Result: Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione上下游产品信息
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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione 试剂级价格
  • 更新日期:2024/04/30
  • 产品编号:HY-116304
  • 产品名称:1G244
  • CAS编号:
  • 包装:1 mg
  • 价格:318元
  • 更新日期:2024/04/30
  • 产品编号:HY-116304
  • 产品名称:(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione 1G244
  • CAS编号:847928-32-9
  • 包装:5mg
  • 价格:700元
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione生产厂家
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