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

Ribociclib hydrochloride  (Synonyms: 瑞博西尼盐酸盐; LEE011 hydrochloride)

目录号: HY-15777A 纯度: 99.88%
Data Sheet SDS COA 产品使用指南 技术支持

溶解度

动物溶解方案

Ribociclib hydrochloride (LEE011 hydrochloride) 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 hydrochloride Chemical Structure

Ribociclib hydrochloride Chemical Structure

CAS No. : 1211443-80-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥725
In-stock
2 mg ￥450
In-stock
5 mg ￥600
In-stock
10 mg ￥960
In-stock
50 mg ￥2500
In-stock
100 mg ￥4150
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of Ribociclib hydrochloride:

Ribociclib hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 60 篇科研文献

WB

    Ribociclib hydrochloride purchased from MCE. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22.  [Abstract]

    Head-to-head comparison of the effect of PD 0332991 and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.

    Ribociclib hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride (LEE011 hydrochloride) 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 hydrochloride 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
    NCT NumberSponsorConditionStart DatePhase
    NCT03050398Novartis Pharmaceuticals|Novartis
    Breast Cancer
    		June 7, 2017Phase 3
    NCT05163106University Hospital, Akershus|Novartis|Vestre Viken Hospital Trust
    Breast Cancer|HER2-negative Breast Cancer|ER-positive Breast Cancer|Locally Advanced Breast Cancer|Luminal A Breast Cancer|Luminal B Breast Cancer
    		December 1, 2022Phase 2
    NCT05161195Novartis Pharmaceuticals|Novartis
    Metastatic Breast Cancer
    		July 7, 2022Phase 4
    分子量

    471.00

    Formula

    C23H31ClN8O
    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    中文名称

    瑞博西尼盐酸盐；瑞柏司可里布盐酸盐
    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
    细胞实验： 

    H2O 中的溶解度 : 10 mg/mL (21.23 mM; 超声助溶)

    DMSO 中的溶解度 : 7.69 mg/mL (16.33 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 2.1231 mL 10.6157 mL 21.2314 mL
    5 mM 0.4246 mL 2.1231 mL 4.2463 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

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.77 mg/mL (1.63 mM); 澄清溶液

      此方案可获得 ≥ 0.77 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 7.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.77 mg/mL (1.63 mM); 澄清溶液

      此方案可获得 ≥ 0.77 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 7.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配制工作液。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: 1 mg/mL (2.12 mM); 澄清溶液; 超声助溶 (<60°C)

    • 方案 二

      请依序添加每种溶剂： 50% PEG300    50% Saline

      Solubility: 20 mg/mL (42.46 mM); 悬浊液; 超声助溶

    扫码获得
    动物溶解方案

    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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， PEG300/PEG400，Tween 80，均可在 MCE 网站选购。
    纯度 & 产品资料

    纯度： 99.95%

    Data Sheet (624 KB) SDS (788 KB)

    COA (286 KB)LCMS (135 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 hydrochloride 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
    DMSO / H2O 1 mM 2.1231 mL 10.6157 mL 21.2314 mL 53.0786 mL
    5 mM 0.4246 mL 2.1231 mL 4.2463 mL 10.6157 mL
    10 mM 0.2123 mL 1.0616 mL 2.1231 mL 5.3079 mL
    15 mM 0.1415 mL 0.7077 mL 1.4154 mL 3.5386 mL
    H2O 20 mM 0.1062 mL 0.5308 mL 1.0616 mL 2.6539 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。

    Keywords:

    Ribociclib1211443-80-9LEE011瑞博西尼盐酸盐瑞柏司可里布盐酸盐LEE 011LEE-011CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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    目录号：
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