2. Cell Cycle/DNA Damage
  3. CDK
  4. Ribociclib succinate

Ribociclib succinate  (Synonyms: 瑞博西尼琥珀酸盐; LEE011 succinate)

目录号: HY-15777B 纯度: 99.93%
COA 产品使用指南

摩尔计算器

Ribociclib succinate (LEE011 succinate) 是一种高度特异性的 CDK4/6 抑制剂，IC50 值分别为 10 nM 和 39 nM，对 cyclin B/CDK1 复合体的活性低于其 1000 倍。

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Ribociclib succinate Chemical Structure

Ribociclib succinate Chemical Structure

CAS No. : 1374639-75-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥730
In-stock
2 mg ￥560
In-stock
5 mg ￥600
In-stock
10 mg ￥840
In-stock
50 mg ￥1440
In-stock
100 mg ￥2160
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Ribociclib succinate:

Ribociclib succinate 相关抗体

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 51 篇科研文献

WB

    Ribociclib succinate purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM for 72 h.

    Ribociclib succinate purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

    Ribociclib succinate purchased from MCE. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59.  [Abstract]

    Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.

    Ribociclib succinate purchased from MCE. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59.  [Abstract]

    Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.

    查看 CDK 亚型特异性产品:

    查看所有亚型
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

    IC50 & Target[1]

    CDK4

    10 nM (IC50)

    CDK6

    39 nM (IC50)

    体外研究
    (In Vitro)

    Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively[2].

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

    Ribociclib succinate 相关抗体:
    体内研究
    (In Vivo)

    CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with Ribociclib (LEE011; 200 mg/kg) or with a vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment[2].

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

    552.63

    Formula

    C27H36N8O5
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    瑞博西尼琥珀酸盐；瑞柏司可里布琥珀酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 9.38 mg/mL (16.97 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : 4.17 mg/mL (7.55 mM; 超声助溶 (<60°C))

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8095 mL 9.0476 mL 18.0953 mL
    5 mM 0.3619 mL 1.8095 mL 3.6191 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 (sealed storage, away from moisture)。-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。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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

    In Vivo:

    以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： PBS

      Solubility: 3.12 mg/mL (5.65 mM); 澄清溶液; 超声助溶 (<60°C)

    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

    纯度: 99.93%

    COA (267 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Cells are grown for 24 hours in 35 mm plates, treated with 500 nM Ribociclib for 6 days, and then fixed and stained overnight. Cells are then imaged for SA-β-gal using an Axio Observer D.1 phase contrast microscope. The percentage of SA-β-gal positive cells is determined by counting the number of positive cells present in three separate microscope frames, and then normalizing to the control. To assess apoptotic activity, cells are plated in triplicate in 96 well plates, treated with Ribociclib, and assayed for caspase 3/7 activation 16 hours after treatment with Caspase-Glo 3/7. Cells treated with SN-38 are used as a positive control[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    The BE2C, NB-1643, or EBC1 cell line-derived xenografts are implanted subcutaneously into the right flank of CB17 SCID-/- mice. Animals bearing engrafted tumors of 200-600 mm3 are then randomized to oral treatment with 200 mg/kg Ribociclib in 0.5 % methylcellulose (n=10) or vehicle (n=10) daily for a total of 21 days. Tumor burden is determined periodically throughout treatment according to the formula (π/6)×d2, where d represents the mean tumor diameter obtained by caliper measurement.

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

    Ribociclib succinate 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 (sealed storage, away from moisture)。-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
    H2O / DMSO 1 mM 1.8095 mL 9.0476 mL 18.0953 mL 45.2382 mL
    5 mM 0.3619 mL 1.8095 mL 3.6191 mL 9.0476 mL
    DMSO 10 mM 0.1810 mL 0.9048 mL 1.8095 mL 4.5238 mL
    15 mM 0.1206 mL 0.6032 mL 1.2064 mL 3.0159 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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:

    Ribociclib1374639-75-4LEE011瑞博西尼琥珀酸盐瑞柏司可里布琥珀酸盐LEE 011LEE-011CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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    目录号：
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