1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis
  3. Dinaciclib

Dinaciclib  (Synonyms: SCH 727965)

目录号: HY-10492 纯度: 99.44%
COA 产品使用指南

Dinaciclib (SCH 727965) 是一种有效的选择性 CDK 抑制剂,抑制 CDK2CDK5CDK1CDK9IC50 分别为 1 nM,1 nM,3 nM 和 4 nM。

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Dinaciclib Chemical Structure

Dinaciclib Chemical Structure

CAS No. : 779353-01-4

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10 mM * 1 mL in DMSO ¥1056
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MCE 顾客使用本产品发表的 32 篇科研文献

Proliferation Assay
WB

    Dinaciclib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2020 Feb;19(2):627-636.  [Abstract]

    Human melanoma cells were treated with Dinaciclib at the indicated doses for 72 hours. After 72-hours incubation, cell viability is assessed by the CellTiter-Glo 2.0 assay. Relative growth to vehicle control is shown.

    Dinaciclib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2020 Feb;19(2):627-636.  [Abstract]

    A2058 melanoma cells are treated with 50 nM Dinaciclib for 3 or 6 hours. Whole cell lysates are subjected to Western blotting (left).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively[1].

    IC50 & Target[1]

    CDK2

    1 nM (IC50)

    CDK5

    1 nM (IC50)

    CDK1

    3 nM (IC50)

    CDK9

    4 nM (IC50)

    体外研究
    (In Vitro)

    Dinaciclib (SCH 727965) 是一种有效的 DNA 复制抑制剂,可阻断 A2780 细胞中胸苷 (dThd) DNA 的掺入,IC50 为 4 nM。Dinaciclib (100 nM) 抑制视网膜母细胞瘤 (Rb) 肿瘤抑制蛋白的磷酸化并诱导 p85 PARP caspase 裂解产物的积累[1]
    Dinaciclib (SCH727965) 以剂量依赖性方式抑制胰腺癌细胞的体外细胞生长。与 Dinaciclib 孵育 72 小时后,MIAPaCa-2 和 Pa20C 细胞的 GI50 分别约为 10 和 20 nM。这些结果与 Dinaciclib 在其他癌细胞系中的研究一致。在软琼脂试验中,5 至 10 nM 的 Dinaciclib 显著减少 MIAPaCa-2 细胞的集落形成和不依赖锚定的生长。Dinaciclib 浓度从 2-5 nM 开始显著降低了 Pa20C 和 MIAPaCa-2 细胞的体外细胞迁移,如使用 BD FluoroChrom、改进的 Boyden Chamber 和伤口愈合测定所证明的那样[2]

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

    体内研究
    (In Vivo)

    Dinaciclib (8、16、32 和 48 mg/kg,ip) 分别导致 70%、70%、89% 和 96% 的肿瘤抑制;Dinaciclib (SCH 727965) 耐受性良好,最高剂量组的最大体重减轻为 5%。Dinaciclib 在小鼠中的血浆半衰期较短。在小鼠中腹腔注射;给予 5 mg/kg 剂量的 Dinaciclib 与约 0.25 小时的血浆半衰期相关[1]。用 Dinaciclib (SCH727965) 进行处理,每周两次 40 mg/kg 的腹腔注射;剂量,持续 4 周,在 10/10 (100%) 的低传代皮下胰腺异种移植物测试中引起显著的肿瘤生长抑制 (TGI)[2]

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

    Clinical Trial
    分子量

    396.49

    Formula

    C21H28N6O2

    CAS 号
    性状

    固体

    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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (126.11 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 2.5221 mL 12.6107 mL 25.2213 mL
    5 mM 0.5044 mL 2.5221 mL 5.0443 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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

    In Vivo:

    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: ≥ 2.5 mg/mL (6.31 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.31 mM); 悬浊液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):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: 20% HP-β-CD in Saline

      Solubility: 10 mg/mL (25.22 mM); 澄清溶液; 超声助溶

    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

    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 ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.44%

    参考文献
    Kinase Assay
    [1]

    Recombinant cyclin/CDK holoenzymes are purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes are typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 1 mM DTT, and 0.1 mM sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2 μM substrate solution (a biotinylated peptide derived from histone H1) are mixed and combined with 10 μL of diluted Dinaciclib (SCH 727965). The reaction is started by the addition of 50 μL of 2 μM ATP and 0.1 μCi of 33P-ATP. Kinase reactions are incubated for 1 hour at room temperature and are stopped by the addition of 0.1% Triton X-100, 1 mM ATP, 5 mM EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads are captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads are washed twice with 2 M NaCl and twice with 2 M NaCl containing 1% phosphoric acid. The signal is then assayed using a TopCount 96-well liquid scintillation counter. Dose-response curves are generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC50 values are derived by nonlinear regression analysis[1].

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

    Cell Assay
    [1]

    A2780 cells are plated onto tissue culture dishes and propagated with the appropriate growth media. Growing cultures are exposed to increasing concentrations of Dinaciclib (0.75, 1.5, 3.15, 6.25, 12.5, 25, and 500 nM) or a vehicle control, typically for 7 days. After removing the medium, cells are fixed with 50% methanol/50% acetone for 5 minutes and stained with 0.2% crystal violet in 2% ethanol for 5 minutes. Following staining, cells are washed with 5 to 10 mL of water. Stained cells are solubilized in 1% deoxycholic acid, and the absorbance of the resulting solution is measured at 600 nm using a SOFTmax PRO 4.3 plate reader. Absorbance of Dinaciclib-treated samples is plotted as a percent of that of a vehicle-treated control, and data are reported as an IC50 value relative to these controls. For suspension cell lines, assessments of cell viability are obtained using the alamarBlue Cell Viability Assay kit[1].

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

    Animal Administration
    [1]

    Mice[1]
    For tumor implantation, specific cell lines are grown in vitro, washed once with PBS, and resuspended in 50% Matrigel in PBS to a final concentration of 4×107 to 5×107 cells per milliliter. Nude mice are injected with 0.1 mL of this suspension s.c. in the flank region. Tumor length (L), width (W), and height (H) are measured by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L×W×H)/2. When the tumor volume reaches 100 mm3, the animals are randomized to treatment groups (10 mice/group) and treated i.p. with either Dinaciclib (8, 16, 32, and 48 mg/kg daily, i.p.) or individual chemotherapeutic agents according to the dosing schedule indicated in table and figure legends. Tumor volumes and body weights are measured during and after the treatment periods.

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

    参考文献

    Dinaciclib 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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 2.5221 mL 12.6107 mL 25.2213 mL 63.0533 mL
    5 mM 0.5044 mL 2.5221 mL 5.0443 mL 12.6107 mL
    10 mM 0.2522 mL 1.2611 mL 2.5221 mL 6.3053 mL
    15 mM 0.1681 mL 0.8407 mL 1.6814 mL 4.2036 mL
    20 mM 0.1261 mL 0.6305 mL 1.2611 mL 3.1527 mL
    25 mM 0.1009 mL 0.5044 mL 1.0089 mL 2.5221 mL
    30 mM 0.0841 mL 0.4204 mL 0.8407 mL 2.1018 mL
    40 mM 0.0631 mL 0.3153 mL 0.6305 mL 1.5763 mL
    50 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2611 mL
    60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0509 mL
    80 mM 0.0315 mL 0.1576 mL 0.3153 mL 0.7882 mL
    100 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6305 mL
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    目录号:
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