1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis
  3. Ro-3306

Ro-3306 是一种有效,选择性的 CDK1 抑制剂,对 CDK1,CDK1/cyclin B1 和 CDK2/cyclin E 的 Ki 值为分别为 20 nM,35 nM 和 340 nM。

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Ro-3306 Chemical Structure

Ro-3306 Chemical Structure

CAS No. : 872573-93-8

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10 mM * 1 mL in DMSO ¥825
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5 mg ¥741
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10 mg ¥1030
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50 mg ¥2800
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Customer Review

MCE 顾客使用本产品发表的 37 篇科研文献

WB

    Ro-3306 purchased from MCE. Usage Cited in: Oncogene. 2018 May;37(19):2601-2614.  [Abstract]

    HEK-293T cells are treated with the ERK1/2 inhibitor SCH772984 (0.5 µM) and/or the CDK1 inhibitor RO-3306 (9 μM) during the last 18 h of transfection. Cells are lysed after 24 h and western blot is performed with the indicated antibodies. HSP90 is used as a loading control.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.

    IC50 & Target[1]

    CDK1

    20 nM (Ki)

    CDK1/cyclinB1

    35 nM (Ki)

    CDK1/cyclin A

    110 nM (Ki)

    CDK2/cyclinE

    340 nM (Ki)

    PKCδ

    318 nM (Ki)

    SGK

    497 nM (Ki)

    ERK

    1980 nM (Ki)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 IC50
    3.2 μM
    Compound: RO3306
    Cytotoxicity against human HCT116 cells after 5 days by MTS assay
    Cytotoxicity against human HCT116 cells after 5 days by MTS assay
    [PMID: 22326168]
    Sf9 IC50
    > 20 μM
    Compound: RO3306
    Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    0.047 μM
    Compound: RO3306
    Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    0.186 μM
    Compound: RO3306
    Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    0.815 μM
    Compound: RO3306
    Inhibition of GST-tagged AURORA B (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate
    Inhibition of GST-tagged AURORA B (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate
    [PMID: 30234987]
    Sf9 IC50
    1.3 μM
    Compound: RO3306
    Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate
    Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate
    [PMID: 30234987]
    Sf9 IC50
    14.5 μM
    Compound: RO3306
    Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    17.4 μM
    Compound: RO3306
    Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    2.48 μM
    Compound: RO3306
    Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    体外研究
    (In Vitro)

    RO-3306 是一种 ATP 竞争性抑制剂,可抑制 CDK1/细胞周期蛋白 A 复合物,Ki 为 110 nM。RO-3306 可阻断人类癌细胞 G2/M 期的细胞周期。RO-3306 (4 μM) 可诱导癌细胞凋亡[1]。RO-3306 (5 μM) 以时间依赖性方式诱导 G2/M 期细胞周期停滞和 AML 细胞凋亡。RO-3306 治疗可显著增加 G1 期细胞中 Annexin V 阳性细胞的百分比,而不会影响细胞周期分布。RO-3306 可增强 p53 介导的细胞凋亡。RO-3306 与 Nutlin-3 协同激活 Bax 并诱导线粒体凋亡。RO-3306 (5 μM) 下调 AML 中的抗凋亡 p21、Bcl-2 和 survivin 蛋白表达。RO-3306 抑制 p53 诱导的 p21 合成。RO-3306 不抑制 RNA 聚合酶 II CTD 磷酸化[2]。RO-3306 (10 μM) 可有效抑制卵母细胞成熟。RO-3306 可减少卵母细胞中的囊胚形成[3]

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

    分子量

    351.45

    Formula

    C18H13N3OS2

    CAS 号
    性状

    固体

    颜色

    Yellow to brown

    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
    细胞实验: 

    DMSO 中的溶解度 : 25 mg/mL (71.13 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 2.8454 mL 14.2268 mL 28.4535 mL
    5 mM 0.5691 mL 2.8454 mL 5.6907 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 year; -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

    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: ≥ 1.67 mg/mL (4.75 mM); 澄清溶液

      此方案可获得 ≥ 1.67 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 16.7 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: ≥ 1.67 mg/mL (4.75 mM); 悬浊液

      此方案可获得 ≥ 1.67 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 16.7 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: 0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (14.23 mM); 悬浊液; 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: 98.68%

    参考文献
    Kinase Assay
    [1]

    The CDK assays are run by using recombinant human CDK/cyclin complexes (CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D) expressed and isolated from Hi5 insect cells. GST-cyclin B1, CDK1, GST-cyclin-E, CDK2, GST-CDK4, and cyclin D, are used in the assay. The GST-tagged proteins are coexpressed and purified in complex with their partners. All assays use a His-6-tagged fragment of pRB (amino acids 385-928) as a substrate. The protein is expressed from a construct. It is expressed in M15 Escherichia coli cells and bound on a Ni-chalated agarose column pretreated with 1 mM imidazole and eluted with 500 mM imidazole. The eluted protein is dialyzed against 20 mM Hepes, pH 7/6.25 mM MgCl2/1.5 mM DTT, aliquoted, and stored at −80°C.

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

    参考文献

    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 year; -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 2.8454 mL 14.2268 mL 28.4535 mL 71.1339 mL
    5 mM 0.5691 mL 2.8454 mL 5.6907 mL 14.2268 mL
    10 mM 0.2845 mL 1.4227 mL 2.8454 mL 7.1134 mL
    15 mM 0.1897 mL 0.9485 mL 1.8969 mL 4.7423 mL
    20 mM 0.1423 mL 0.7113 mL 1.4227 mL 3.5567 mL
    25 mM 0.1138 mL 0.5691 mL 1.1381 mL 2.8454 mL
    30 mM 0.0948 mL 0.4742 mL 0.9485 mL 2.3711 mL
    40 mM 0.0711 mL 0.3557 mL 0.7113 mL 1.7783 mL
    50 mM 0.0569 mL 0.2845 mL 0.5691 mL 1.4227 mL
    60 mM 0.0474 mL 0.2371 mL 0.4742 mL 1.1856 mL
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    产品名称:
    Ro-3306
    目录号:
    HY-12529
    需求量: