1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. SCH900776

SCH900776  (Synonyms: MK-8776)

目录号: HY-15532 纯度: 99.92%
COA 产品使用指南

SCH900776 (MK-8776) 是一种有效,选择性,可口服的 Chk1 抑制剂,IC50 值为 3 nM;它比对CDK2 和 Chk2 的选择性分别高 50 和 500 倍。

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SCH900776 Chemical Structure

SCH900776 Chemical Structure

CAS No. : 891494-63-6

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1281
In-stock
2 mg ¥1032
In-stock
5 mg ¥1548
In-stock
10 mg ¥2727
In-stock
50 mg ¥7149
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of SCH900776:

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Top Publications Citing Use of Products

    SCH900776 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688.  [Abstract]

    EW8 cells are treated with 50 nM LY 188011 in combination with increasing doses of Prexasertib, LY2603618, or MK-8776 for 6 hours. Cell lysates are then collected and blotted for p-CHK1- 296.

    查看 Checkpoint Kinase (Chk) 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively[1][2].

    IC50 & Target[2]

    Chk1

    3 nM (IC50)

    Chk2

    1500 nM (IC50)

    CDK2

    160 nM (IC50)

    体外研究
    (In Vitro)

    SCH900776 (300 nM) 对 ser296-Chk1 的磷酸化表现出有效的抑制活性。SCH900776 (1 μM) 导致 MDA-MB-231 细胞中 NSC-32065 的 IC50 降低 30 倍[1]。SCH 900776 对 CHK1 激酶结构域的 Kd 值为 2 nM。SCH 900776 在暴露于 NSC-32065 的细胞中表现出大约 60 nM 的 EC50。SCH 900776 在 U2OS 细胞中诱导 CHK1 pS296 的剂量依赖性抑制和磷酸化 RPA 信号的伴随积累[2]

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

    体内研究
    (In Vivo)

    SCH 900776 以 4 mg/kg (i.p.) 诱导 γ-H2AX 生物标志物,并增强 A2780 异种移植模型中的肿瘤药效学和消退反应。 SCH 900776(16 和 32 mg/kg,腹腔注射)诱导肿瘤反应的逐步改善。 将 SCH 900776 剂量增加至 20 和 50 mg/kg 并与 LY 188011 联合使用可使 A2780 异种移植系统中的 TTP 提高 10 倍[2]

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

    Clinical Trial
    分子量

    376.25

    Formula

    C15H18BrN7

    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 : ≥ 100 mg/mL (265.78 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6578 mL 13.2890 mL 26.5781 mL
    5 mM 0.5316 mL 2.6578 mL 5.3156 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 (6.64 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 (6.64 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 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。
    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: 99.97%

    参考文献
    Kinase Assay
    [2]

    The Kinase Profiler service is used to generate general selectivity data for SCH 900776 against a broad range of serine/threonine and tyrosine kinases. Assays are typically run at two concentrations of SCH 900776 (0.5 and 5 μM), at a fixed (10 μM) concentration of ATP.

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

    Cell Assay
    [1]

    For cell growth assays, cells are seeded at low density (500-1000 cells) in 96-well plates and then incubated with drug for 24 h (8 wells per concentration). Following treatment, cells are washed and grown in fresh media for 5-7 days at 37°C. Prior to attaining confluence, cells are washed, lysed, and stained with Hoechst 33258. Fluorescence is read on a microplate spectrofluorometer. Results are expressed as mean and standard error for the concentration of drug that inhibited growth by 50%.

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

    Animal Administration
    [2]

    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 mL. Nude mice are injected with 0.1 mL of this suspension subcutaneously in the flank region. Tumor length (L), width (W), and height (H) are measured by a caliper twice a week on each mouse and then used to calculate tumor volume using the formula: (L×W×H)/2. Animals (N=10) are randomized to treatment groups and treated intraperitoneally with either SCH 900776 (formulated in 20% hydroxypropyl β-cyclodextrin) or individual chemotherapeutic agents, formulated as recommended. Tumor volumes and body weights are measured during and after the treatment periods. Data are recorded as means±SEM before being normalized to starting volume. Time to progression to 10x starting volume (TTP 10x) is monitored in some experiments. For pharmacodynamic marker analyses in mice, tumors and adjacent skin are collected at necropsy, fixed overnight in 10% formalin, and washed/stored in 70% ethanol. For skin punch biopsies, an area of approximately 4 square inches is shaved. Rats are anesthetized using inhaled isofluorane and dogs are locally anesthetized using subcutaneous administration of lidocaine. Samples are collected using a 4 mm biopsy punch. Skin punches are fixed in 10% formalin overnight before washing/storage in 70% ethanol.

    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 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 2.6578 mL 13.2890 mL 26.5781 mL 66.4452 mL
    5 mM 0.5316 mL 2.6578 mL 5.3156 mL 13.2890 mL
    10 mM 0.2658 mL 1.3289 mL 2.6578 mL 6.6445 mL
    15 mM 0.1772 mL 0.8859 mL 1.7719 mL 4.4297 mL
    20 mM 0.1329 mL 0.6645 mL 1.3289 mL 3.3223 mL
    25 mM 0.1063 mL 0.5316 mL 1.0631 mL 2.6578 mL
    30 mM 0.0886 mL 0.4430 mL 0.8859 mL 2.2148 mL
    40 mM 0.0664 mL 0.3322 mL 0.6645 mL 1.6611 mL
    50 mM 0.0532 mL 0.2658 mL 0.5316 mL 1.3289 mL
    60 mM 0.0443 mL 0.2215 mL 0.4430 mL 1.1074 mL
    80 mM 0.0332 mL 0.1661 mL 0.3322 mL 0.8306 mL
    100 mM 0.0266 mL 0.1329 mL 0.2658 mL 0.6645 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.

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    产品名称:
    SCH900776
    目录号:
    HY-15532
    需求量: