2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. TAK-960 dihydrochloride

TAK-960 dihydrochloride 

目录号: HY-15160B 纯度: 99.19%
COA 产品使用指南

摩尔计算器

TAK-960 dihydrochloride 是一种有效的，可口服的，选择性的 polo-like kinase 1 (PLK1) 抑制剂，IC50 为 0.8 nM。TAK-960 dihydrochloride 对 PLK2 和 PLK3 也有抑制作用，IC50 分别为 16.9 和 50.2 nM。TAK-960 dihydrochloride 抑制多种肿瘤细胞系的增殖，对多种肿瘤异种移植具有显著的疗效。

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

TAK-960 dihydrochloride Chemical Structure

TAK-960 dihydrochloride Chemical Structure

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 Water ￥2180
In-stock
5 mg ￥1300
In-stock
10 mg ￥1800
In-stock
50 mg ￥5400
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of TAK-960 dihydrochloride:

TAK-960 dihydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型
PLK1 PLK2 PLK3 PLK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts[1].

IC50 & Target[1]

PLK1

0.8 nM (IC50)

PLK2

16.9 nM (IC50)

PLK3

50.2 nM (IC50)

FAK/PTK2

19.6 nM (IC50)

MLCK/MYLK

25.6 nM (IC50)

FES/FPS

58.2 nM (IC50)

体外研究
(In Vitro)

TAK-960 dihydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 dihydrochloride (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells[1].
TAK-960 dihydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells[2].

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

TAK-960 dihydrochloride 相关抗体:

Cell Viability Assay[1]

Cell Line: HT-29, HCT116, COLO320DM, HCT-15, RKO, SW480, K-562….Hela, DU 145 cells
Concentration: 2-1000 nM
Incubation Time: 72 hours
Result: Inhibited proliferation of human cancer cell lines regardless of TP53 and KRAS mutation and MDR1 expression status.
体内研究
(In Vivo)

TAK-960 dihydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts[1].
In animal models, TAK-960 dihydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts[1].

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

Animal Model: nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)[1]
Dosage: 10 mg/kg
Administration: P.o.; once daily for 2 weeks
Result: Substantial antitumor activity and good tolerability.
Clinical Trial
分子量

634.52

Formula

C27H36Cl2F3N7O3
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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

H2O 中的溶解度 : 10 mg/mL (15.76 mM; 超声助溶)

DMSO 中的溶解度 : 3.23 mg/mL (5.09 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 1.5760 mL 7.8800 mL 15.7599 mL
5 mM 0.3152 mL 1.5760 mL 3.1520 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 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

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
纯度 & 产品资料
参考文献

TAK-960 dihydrochloride 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1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 / H2O 1 mM 1.5760 mL 7.8800 mL 15.7599 mL 39.3999 mL
5 mM 0.3152 mL 1.5760 mL 3.1520 mL 7.8800 mL
H2O 10 mM 0.1576 mL 0.7880 mL 1.5760 mL 3.9400 mL
15 mM 0.1051 mL 0.5253 mL 1.0507 mL 2.6267 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:

TAK-960TAK960TAK 960Polo-like Kinase (PLK)proliferationcancercelllinesleukemiamitosisphosphorylationInhibitorinhibitorinhibit

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：
TAK-960 dihydrochloride
目录号：
HY-15160B
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