2. Cell Cycle/DNA Damage
  3. CDK
  4. BS-181 hydrochloride

BS-181 hydrochloride 

目录号: HY-13266A 纯度: 99.80%
COA 产品使用指南

摩尔计算器

BS-181 hydrochloride 是一种高度选择性的 CDK7 抑制剂，IC50 值为 21 nM，对 CDK7 的选择性是对 CDK1，2，4，5，6 和 9 的 40 多倍。

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BS-181 hydrochloride Chemical Structure

BS-181 hydrochloride Chemical Structure

CAS No. : 1397219-81-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥880
In-stock
5 mg ￥800
In-stock
10 mg ￥1100
In-stock
25 mg ￥2300
In-stock
50 mg ￥3500
In-stock
100 mg ￥5400
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of BS-181 hydrochloride:

BS-181 hydrochloride 相关抗体

Top Publications Citing Use of Products

    BS-181 hydrochloride purchased from MCE. Usage Cited in: Theranostics. 2017 Apr 20;7(7):1914-1927.  [Abstract]

    Effect of TPL on the levels of pAR S515 and related proteins in PCa cells. LNCaP and C4-2/AR-V7 cells are pretreated with TPL or BS-181 for 1 h, and then incubated with R1881 for 4 h.

    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

    BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

    IC50 & Target[1]

    CDK7/CycH/MAT1

    0.021 μM (IC50)

    CDK2/Cyc E

    0.88 μM (IC50)

    CDK5/p35NCK

    3 μM (IC50)

    CDK9/cycT

    4.2 μM (IC50)

    CDK1/cycB

    8.1 μM (IC50)

    CDK4/Cyc D1

    33 μM (IC50)

    CDK6/cycD1

    47 μM (IC50)

    体外研究
    (In Vitro)

    BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC50 values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser795 and Ser821 with an apparent IC50 of 15 μM, similar to the IC50 obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis[1]. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC50) ranging from 17 to 22 μM and 6.5 μM, respectively. BS-181 significantly inhibits cell migration and invasion ability in a dose-dependent manner[2].

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

    BS-181 hydrochloride 相关抗体:
    体内研究
    (In Vivo)

    BS-181 (5 mg/kg, 10 mg/kg, i.p.) inhibits the growth of MCF-7 tumors in nude mice. Intravenous (i.v) and i.p administration of 10 mg/kg BS-181 shows rapid clearance[1]. BS-181 (10 mg/kg/d or 20 mg/kg/d, i.p.) significantly inhibits the growth of tumor in a dose-dependent manner compared to the control group[2].

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

    416.99

    Formula

    C22H33ClN6
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 100 mg/mL (239.81 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 50 mg/mL (119.91 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 2.3981 mL 11.9907 mL 23.9814 mL
    5 mM 0.4796 mL 2.3981 mL 4.7963 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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    * 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:

    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: ≥ 3 mg/mL (7.19 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (7.19 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 30.0 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： PBS

      Solubility: 50 mg/mL (119.91 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

    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
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料
    参考文献
    Cell Assay
    [2]

    Cell viability is detected using Cell Counting Kit (CCK-8 kit) according to supplier’s introductions. Briefly, BGC823 cells are seeded at 104 cells per well for 48 hours with or without BS-181. Then, the absorbance is detected at 450 nm (reference at 650 nm) in each well.

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

    In total, 5×106 BGC823 cells (0.1 mL) are injected subcutaneously into the flank of the mice. Tumor measurements are performed two times per week, and volumes are calculated using the formula: tumor size=(length ×width2)/2. Finally, 30 mice (tumor volume 100-200 mm3) are selected and randomLy assigned into three groups. As previously described, BS-181 is prepared in 10% dimethyl sulfoxide/50 mM HCl/5% Tween 20/85% saline. Micereceive BS-181 injection (ip) twice daily at indicated doses (BS-181 [10 mg/kg/d or 20 mg/kg/d] or Roscovitine [20 mg/kg/d]) for a total of 14 days. Control mice are injected with vehicles. Animal weights and tumor volume are measured each day throughout the 14-day treatment. In addition, all rats are kept for another 30 days for survival observation. Mice are injected intraperitoneally twice daily with BS-181 at 5 mg/kg or 10 mg/kg.

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

    BS-181 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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 2.3981 mL 11.9907 mL 23.9814 mL 59.9535 mL
    5 mM 0.4796 mL 2.3981 mL 4.7963 mL 11.9907 mL
    10 mM 0.2398 mL 1.1991 mL 2.3981 mL 5.9953 mL
    15 mM 0.1599 mL 0.7994 mL 1.5988 mL 3.9969 mL
    20 mM 0.1199 mL 0.5995 mL 1.1991 mL 2.9977 mL
    25 mM 0.0959 mL 0.4796 mL 0.9593 mL 2.3981 mL
    30 mM 0.0799 mL 0.3997 mL 0.7994 mL 1.9984 mL
    40 mM 0.0600 mL 0.2998 mL 0.5995 mL 1.4988 mL
    50 mM 0.0480 mL 0.2398 mL 0.4796 mL 1.1991 mL
    60 mM 0.0400 mL 0.1998 mL 0.3997 mL 0.9992 mL
    80 mM 0.0300 mL 0.1499 mL 0.2998 mL 0.7494 mL
    100 mM 0.0240 mL 0.1199 mL 0.2398 mL 0.5995 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:

    BS-1811397219-81-6BS181BS 181CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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