2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase
  4. CYC-116

CYC-116是有效的极光激酶A和B (aurora A/B) 的抑制剂，Ki 值分别为8和9 nM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

CYC-116 Chemical Structure

CYC-116 Chemical Structure

CAS No. : 693228-63-6

1.  客户无需承担相应的运输费用。

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 ￥550
In-stock
5 mg ￥500
In-stock
10 mg ￥800
In-stock
50 mg ￥2600
In-stock
100 mg ￥4500
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

CYC-116 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

CYC-116 is a potent aurora A and aurora B inhibitor with Kis of 8 and 9 nM, respectively.

IC50 & Target[1]

Aurora A

8 nM (Ki)

Aurora B

9.2 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
170 nM
Compound: 18, CYC-116
Cytotoxicity against human A2780 cells after 96 hrs by MTT assay
Cytotoxicity against human A2780 cells after 96 hrs by MTT assay
[PMID: 20462263]
A549 IC50
0.48 μM
Compound: 18, CYC-116
Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy
Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy
[PMID: 20462263]
BXPC-3 IC50
1.626 μM
Compound: 18, CYC-116
Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay
Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay
[PMID: 20462263]
CCRF-CEM IC50
0.471 μM
Compound: 18, CYC-116
Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay
Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay
[PMID: 20462263]
COLO 205 IC50
0.241 μM
Compound: 18, CYC-116
Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay
Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay
[PMID: 20462263]
HCT-116 IC50
0.34 μM
Compound: 18, CYC-116
Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay
[PMID: 20462263]
HeLa IC50
0.59 μM
Compound: 18, CYC-116
Cytotoxicity against human HeLa cells after 96 hrs by MTT assay
Cytotoxicity against human HeLa cells after 96 hrs by MTT assay
[PMID: 20462263]
HL-60 IC50
0.372 μM
Compound: 18, CYC-116
Cytotoxicity against human HL60 cells after 96 hrs by MTT assay
Cytotoxicity against human HL60 cells after 96 hrs by MTT assay
[PMID: 20462263]
HT-29 IC50
0.725 μM
Compound: 18, CYC-116
Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay
[PMID: 20462263]
HuP-T4 IC50
0.775 μM
Compound: 18, CYC-116
Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay
Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay
[PMID: 20462263]
K562 IC50
1.375 μM
Compound: 18, CYC-116
Cytotoxicity against human K562 cells after 96 hrs by MTT assay
Cytotoxicity against human K562 cells after 96 hrs by MTT assay
[PMID: 20462263]
MCF7 IC50
0.599 μM
Compound: 18, CYC-116
Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay
[PMID: 20462263]
MES-SA IC50
0.09 μM
Compound: 18, CYC-116
Cytotoxicity against human MESSA cells after 96 hrs by MTT assay
Cytotoxicity against human MESSA cells after 96 hrs by MTT assay
[PMID: 20462263]
MIA PaCa-2 IC50
278 nM
Compound: 18, CYC-116
Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay
[PMID: 20462263]
MV4-11 IC50
0.034 μM
Compound: 18, CYC-116
Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay
Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay
[PMID: 20462263]
NCI-H460 IC50
0.681 μM
Compound: 18, CYC-116
Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay
Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay
[PMID: 20462263]
SAOS-2 IC50
0.11 μM
Compound: 18, CYC-116
Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay
Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay
[PMID: 20462263]
体外研究
(In Vitro)

CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. CYC-116 shows potent antiproliferative activity against cancer cell lines with with IC50s of 0.599, 0.59, 0.241, 0.34, 0.725, 1.375, 0.471, 0.034, 0.372, 0.681, 0.151, 1.626, 0.775, 0.308, 0.110, 0.09 for MCF7, HeLa, Colo205, HCT-116, HT29, K562, CCRF-CEM, MV4-11, HL60, NCI-H460, A2780, BxPC3, HuPT4, Mia-Paca-2, Saos-2, Messa cells. Treatment with 1.25 μM CYC-116 for 7 h results in complete inhibition of histone H3 phosphorylation in HeLa cell lysates[1].

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

CYC-116 相关抗体:
体内研究
(In Vivo)

Oral administration of CYC-116 at dose levels of 75 and 100 mg/kg q.d. causes tumor growth delays of 2.3 and 5.8 days, which translates into specific growth delays of 0.32 and 0.81, respectively. The mean relative tumor volumes of mice receiving CYC-116 at both dose levels are less than those of vehicle-treated mice for the duration of the study period. At 100 mg/kg po q.d., the reduction in growth is statistically significant on days 6 and 9[1].

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

368.46

Formula

C18H20N6OS
CAS 号
性状

固体

颜色

Light yellow to yellow

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
细胞实验： 

DMSO 中的溶解度 : 15 mg/mL (40.71 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)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7140 mL 13.5700 mL 27.1400 mL
5 mM 0.5428 mL 2.7140 mL 5.4280 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

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: 1.5 mg/mL (4.07 mM); 悬浊液; 超声助溶

    此方案可获得 1.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 15.0 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: ≥ 1.5 mg/mL (4.07 mM); 澄清溶液

    此方案可获得 ≥ 1.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 15.0 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。

    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

只
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: 98.17%

COA (190 KB) HNMR (165 KB) LCMS (377 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

Aurora A kinase assays are performed using a 25 μL reaction volume (25 mM β-glycerophosphate, 20 mM Tris/HCl, pH 7.5, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO4, 10 μg of kemptide (peptide substrate)), and recombinant aurora A kinase is diluted in 20 mM Tris/HCl, pH 8, containing 0.5 mg/mL BSA, 2.5% glycerol, and 0.006% Brij-35. Reactions are started by the addition of 5 μL Mg/ATP mix (15 mM MgCl4, 100 μM ATP, with 18.5 kBq γ-32P-ATP per well) and incubated at 30°C for 30 min before terminating by the addition of 25 μL of 75 mM H3PO4. Aurora B kinase assays are performed as for aurora A except that prior to use, aurora B is activated in a separate reaction at 30°C for 60 min with inner centromeres protein[1].

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

CYC-116 is prepared in DMSO and diluted in cell medium[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Mice implanted intraperitoneally with P388/0 cells are treated with CYC-116, and the antitumor activity is measured as an increase in lifespan of the treated animals versus the vehicle control group[1].

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

CYC-116 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 2.7140 mL 13.5700 mL 27.1400 mL 67.8500 mL
5 mM 0.5428 mL 2.7140 mL 5.4280 mL 13.5700 mL
10 mM 0.2714 mL 1.3570 mL 2.7140 mL 6.7850 mL
15 mM 0.1809 mL 0.9047 mL 1.8093 mL 4.5233 mL
20 mM 0.1357 mL 0.6785 mL 1.3570 mL 3.3925 mL
25 mM 0.1086 mL 0.5428 mL 1.0856 mL 2.7140 mL
30 mM 0.0905 mL 0.4523 mL 0.9047 mL 2.2617 mL
40 mM 0.0678 mL 0.3392 mL 0.6785 mL 1.6962 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.

Keywords:

CYC-116693228-63-6CYC116CYC 116Aurora KinaseInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
CYC-116
目录号：
HY-10558
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z