2. JAK/STAT Signaling Apoptosis
  3. Pim Apoptosis
  4. PIM447

PIM447  (Synonyms: LGH447)

目录号: HY-19322 纯度: 99.78%
COA 产品使用指南

摩尔计算器

PIM447 (LGH447) 是一种有效的、口服的、选择性的泛 PIM 激酶抑制剂，对 PIM1、PIM2 和 PIM3 的 Ki 值分别为 6、18 和 9 pM。PIM447 具有双重抗肿瘤和骨保护作用。PIM447 诱导细胞凋亡。

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PIM447 Chemical Structure

PIM447 Chemical Structure

CAS No. : 1210608-43-7

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
1 mg ￥1363
In-stock
5 mg ￥3000
In-stock
10 mg ￥4800
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of PIM447:

PIM447 相关抗体

Top Publications Citing Use of Products

    PIM447 purchased from MCE. Usage Cited in: J Pathol. 2020 Sep;252(1):65-76.  [Abstract]

    The alteration of MAPK/ERK pathway is validated by Western blotting with tumour lysates from the animal model, as illustrated by a downregulation of pERK1/2 in the PIM447 treatment group.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis[1][2].

    体外研究
    (In Vitro)

    PIM447 (0.05-10 μM; 24-72 hours) shows antiproliferative effect on the multiple myeloma (MM) cells[2].
    PIM447 (10 μM; 6-24 hours) induces apoptosis[2].
    PIM447 (0.1-10 μM; 48 hours) increases the percentage of cells in the G0-G1 phase and decreases the proliferative phases (S and G2–M) of the cell cycle, in the two cell lines (MM1S and OPM-2 cells) at all doses[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    PIM447 相关抗体:

    Cell Viability Assay[2]

    Cell Line: MM1S, MM1R, RPMI-8226, MM144, U266, NCI-H929, OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7 cells
    Concentration: 0.05, 0.1, 0.5, 1, 5, 10 μM
    Incubation Time: 24, 48, 72 hours
    Result: Sensitive cell lines with IC50 values at 48 hours ranging from 0.2 to 3.3 μM (MM1S, MM1R, RPMI-8226, MM144, U266, and NCI-H929) and less sensitive cell lines with IC50 values at 48 hours >7 μmol/L (OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7).

    Western Blot Analysis[2]

    Cell Line: MM1S cells
    Concentration: 10 μM
    Incubation Time: 6, 12, 24 hours
    Result: Promoted the cleavage of initiator caspases, such as caspases 8 and 9, and also the cleavage of the effector caspases 3 and 7, together with PARP cleavage.
    体内研究
    (In Vivo)

    PIM447 (100 mg/kg; p.o.; 5 times for a week) reduces tumor burden[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 6-week-old female NOD-SCID-IL-2Rγ−/− (NSG) mice (bearing RPMI-8226-luc cells)[2]
    Dosage: 100 mg/kg
    Administration: p.o.; 5 times for a week
    Result: Clearly controlled tumor progression as measured by bioluminescence. 
    Clinical Trial
    分子量

    440.46

    Formula

    C24H23F3N4O
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (227.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2704 mL 11.3518 mL 22.7035 mL
    5 mM 0.4541 mL 2.2704 mL 4.5407 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献

    PIM447 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2704 mL 11.3518 mL 22.7035 mL 56.7588 mL
    5 mM 0.4541 mL 2.2704 mL 4.5407 mL 11.3518 mL
    10 mM 0.2270 mL 1.1352 mL 2.2704 mL 5.6759 mL
    15 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7839 mL
    20 mM 0.1135 mL 0.5676 mL 1.1352 mL 2.8379 mL
    25 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 mL
    30 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
    40 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4190 mL
    50 mM 0.0454 mL 0.2270 mL 0.4541 mL 1.1352 mL
    60 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9460 mL
    80 mM 0.0284 mL 0.1419 mL 0.2838 mL 0.7095 mL
    100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5676 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PIM4471210608-43-7LGH447PIM 447PIM-447LGH 447LGH-447PimApoptosisPim kinasespanantimyelomamultiplemyelomacellcycleapoptosistumorantiproliferativeprogressionbone-protectivehematologicalmalignanciesInhibitorinhibitorinhibit

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    目录号：
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