1. Cell Cycle/DNA Damage Cytoskeleton
  2. Mps1
  3. Empesertib

Empesertib  (Synonyms: BAY 1161909)

目录号: HY-12858 纯度: 98.82%
COA 产品使用指南

Empesertib (BAY 1161909) 是一种有效的 Mps1 抑制剂,IC50 值 <1 nM。

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Empesertib Chemical Structure

Empesertib Chemical Structure

CAS No. : 1443763-60-7

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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 ¥4309
In-stock
2 mg ¥2333
In-stock
5 mg ¥3500
In-stock
10 mg ¥5000
In-stock
50 mg
询价
100 mg
询价

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC50 of < 1 nM.

IC50 & Target

Mps1

1 nM (IC50)

体外研究
(In Vitro)

BAY 1161909 is a potent Mps1 inhibitor, with an IC50 of < 1 nM. BAY 1161909 also shows anti-tumor effect, suppressing the proliferation of Hela cells, with an IC50 of < 400 nM[1].

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

Clinical Trial
分子量

559.61

Formula

C29H26FN5O4S

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 35 mg/mL (62.54 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 1.7870 mL 8.9348 mL 17.8696 mL
5 mM 0.3574 mL 1.7870 mL 3.5739 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。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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 (4.47 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 (4.47 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL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。
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: 98.82%

参考文献
Kinase Assay
[1]

N-terminally GST-tagged human full length recombinant Mps-1 kinase is used. As substrate for the kinase reaction a biotinylated peptide of the amino-acid sequence PWDPDDADITEILG is used. For the assay 50 nL of a 100-fold concentrated solution of the test compounds (BAY 1161909, etc.) in DMSO is pipetted into a black low volume 384 well microtiter plate, 2 μL of a solution of Mps-1 in assay buffer [0.1 mM sodium-ortho-vanadate, 10 mM MgCl2, 2 mM DTT, 25 mM Hepes pH 7.7, 0.05% BSA, 0.001 % Pluronic F-127] are added and the mixture is incubated for 15 min at 22°C to allow pre-binding of the test compounds to Mps-1 before the start of the kinase reaction. Then the kinase reaction is started by the addition of 3 μL of a solution of 16.7 adenosine-tri-phosphate and peptide substrate in assay buffer and the resulting mixture is incubated for a reaction time of 60 min at 22°C. The concentration of Mps-1 in the assay is adjusted to the activity of the enzyme lot and is chosen appropriate to have the assay in the linear range, typical enzyme concentrations are in the range of about 1 nM (final cone, in the 5 μL assay volume). The reaction is stopped by the addition of 3 μL of a solution of HTRF detection reagents (100 mM Hepes pH 7.4, 0.1 % BSA, 40 mM EDTA, 140 nM Streptavidin-XLent, 1 .5 nM anti-phospho(Ser/Thr)-Europium-antibody[1].

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

Cell Assay
[1]

Cultivated tumor cells are plated at a density of 5000 cells/ well (MCF7, DU145, HeLa-MaTu-ADR), 3000 cells/well (NCI-H460, HeLa-MaTu, HeLa), or 1000 cells/well (B16F10) in a 96-well multititer plate in 200 μL of their respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates is replaced by fresh culture medium (200 μL), to which the test substances (BAY 1161909, etc.) are added in various concentrations (0 μM, as well as in the range of 0.01-30 μM; the final concentration of the solvent DMSO is 0.5%). The cells are incubated for 4 days in the presence of test substances. Cell proliferation is determined by staining the cells with crystal violet: the cells are fixed by adding 20 μL/measuring point of an 11% glutaric aldehyde solution for 15 minutes at room temperature. After three washing cycles of the fixed cells with water, the plates are dried at room temperature. The cells are stained by adding 100 μL/measuring point of a 0.1% crystal violet solution (pH 3.0). After three washing cycles of the stained cells with water, the plates are dried at room temperature. The dye is dissolved by adding 100 μL/measuring point of a 10% acetic acid solution. The IC50 values are determined by means of a 4 parameter fit. The compounds A1 (BAY 1161909), A2, A3, A4 and A5 are characterized by an IC50 determined in a HeLa-MaTu-ADR cell proliferation assay[1].

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

参考文献

Empesertib 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。-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 1 mM 1.7870 mL 8.9348 mL 17.8696 mL 44.6740 mL
5 mM 0.3574 mL 1.7870 mL 3.5739 mL 8.9348 mL
10 mM 0.1787 mL 0.8935 mL 1.7870 mL 4.4674 mL
15 mM 0.1191 mL 0.5957 mL 1.1913 mL 2.9783 mL
20 mM 0.0893 mL 0.4467 mL 0.8935 mL 2.2337 mL
25 mM 0.0715 mL 0.3574 mL 0.7148 mL 1.7870 mL
30 mM 0.0596 mL 0.2978 mL 0.5957 mL 1.4891 mL
40 mM 0.0447 mL 0.2234 mL 0.4467 mL 1.1168 mL
50 mM 0.0357 mL 0.1787 mL 0.3574 mL 0.8935 mL
60 mM 0.0298 mL 0.1489 mL 0.2978 mL 0.7446 mL
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    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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