1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. Aurora Kinase CDK Apoptosis
  3. JNJ-7706621

JNJ-7706621 是一种有效的 aurora kinase 抑制剂,同时能有效抑制 CDK1CDK2,对 CDK1CDK2aurora-Aaurora-BIC50 值分别为 9 nM,3 nM,11 nM 和 15 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

JNJ-7706621 Chemical Structure

JNJ-7706621 Chemical Structure

CAS No. : 443797-96-4

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 ¥1215
In-stock
2 mg ¥800
In-stock
5 mg ¥1400
In-stock
10 mg ¥2500
In-stock
50 mg ¥6100
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

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

JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively[1][2][3].

IC50 & Target[3]

CDK6/cyclinD1

175 nM (IC50)

CDK2/cyclinE

3 nM (IC50)

Cdk4/cyclin D1

253 nM (IC50)

Cdk1/cyclin B

9 nM (IC50)

cdk2/cyclin A

4 nM (IC50)

CDK3/Cyclin E

58 nM (IC50)

Aurora A

11 nM (IC50)

Aurora B

15 nM (IC50)

VEGF-R2

154 nM (IC50)

VEGF-R1

6400 nM (IC50)

VEGF-R3

735 nM (IC50)

FGF-R1

575 nM (IC50)

FGF-R2

226 nM (IC50)

GSK3β

254 nM (IC50)

体外研究
(In Vitro)

JNJ-7706621 对多种人类肿瘤细胞具有抗增殖活性,对 HeLa、HCT116 和 A375 的 IC50 分别为 284、254 和 447 nM[1]。JNJ-7706621 在有丝分裂早期抑制其他中心体蛋白,如 TOG、Nek2 和 TACC3,但不会阻止 Aurora A 定位到纺锤体两极。用 JNJ-7706621 处理诺考达唑同步细胞可以通过阻止纺锤体检查点信号传导来克服有丝分裂停滞,从而导致染色体排列和分离失败[2]。JNJ-7706621 显示出对 Aurora-A 和 Aurora-B 的抑制作用,但在对 Plk1Wee1 丝氨酸/苏氨酸激酶测试的最高浓度下没有活性。JNJ-7706621 还在体外对所有人类癌细胞类型显示出有效的生长抑制作用,IC50 值范围为 112 至 514 nM[3]。JNJ-7706621 悬浮液抑制 HeLa 细胞的细胞活力,24 小时和 48 小时的 IC50 分别为 2.1 和 0.9 μg/mL。载有 JNJ-7706621 的纳米粒子的 IC50 分别为 35 和 2.7 μg/mL,载有 JNJ-7706621 的胶束的 IC50 分别为 6.3 和 1.6 μg/mL mL[4]

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

体内研究
(In Vivo)

JNJ-7706621 (100 和 125 mg/kg) 在间歇给药方案下对人肿瘤异种移植模型有效[3]
JNJ-7706621 (100 mg/kg,腹腔注射) 在 A375 (人黑色素瘤) 肿瘤异种移植模型中表现出 95% 的肿瘤生长抑制[1]。JNJ-7706621 负载胶束抑制肿瘤生长,JNJ-7706621 悬浮液比对照组更有效地延缓肿瘤生长[4]

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

分子量

394.36

Formula

C15H12F2N6O3S

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 125 mg/mL (316.97 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 2.5358 mL 12.6788 mL 25.3575 mL
5 mM 0.5072 mL 2.5358 mL 5.0715 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。-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。

  • 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: ≥ 2.08 mg/mL (5.27 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.27 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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: 99.91%

参考文献
Kinase Assay
[4]

To identify compounds that inhibit CDK1 kinase activity, a screening method is developed using the CDK1/cyclin B complex to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylatedin vivo by CDK1. Inhibition of CDK1 activity is measured by observing a reduced amount of 33P-g-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 AM peptide, 0.1 ACi per well 33P-g-ATP (2,000-3,000 Ci/mmol), and 5 AM ATP in the presence or absence of various concentrations of test compound and incubated at 30°C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. Linear regression analysis of the percent inhibition by test compound is used to determine IC50 values. The Aurora kinase assays are done with 10 AM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.

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

Cell Assay
[3]

HeLa cells are seeded in 96-well plates at the density of 2500 viable cells per well. The cells are then incubated with a suspension of JNJ-7706621, JNJ-7706621-loaded micelles and nanoparticles (JNJ-7706621 concentrations of 0.011, 0.022, 0.11, 0.22, 1.1, 2.2, 11 and 22 μg/mL; dilutions are made in the medium) and drug-free polymeric micelles (polymers concentrations 0.3 mg/mL) and nanoparticles (polymers concentration 5 mg/mL) for 4, 24 and 48 h. The cytotoxicity is assessed using the MTT test. Absorbance is measured at 570 nm using a microplate reader. Untreated cells are taken as control with 100% viability and Triton X-100 1% is used as positive control of cytotoxicity. The results are expressed as mean values ± standard deviations of five measurements.

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

Animal Administration
[4]

Briefly, animals are implanted s.c. with 1 mm3 A375 tumor fragments in the hindflank. After tumors reach 62 to 126 mg, groups are pair matched. Animals are given JNJ-7706621 or vehicle control starting on day 1. The tumor growth delay method is followed where each animal is euthanized when its neoplasm reached a predetermined size of 2.0 g. All statistical analyses are conducted using unpaired t tests at a P level of 0.05 (two tailed).

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, 6 months; -20°C, 1 month。-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 1 mM 2.5358 mL 12.6788 mL 25.3575 mL 63.3939 mL
5 mM 0.5072 mL 2.5358 mL 5.0715 mL 12.6788 mL
10 mM 0.2536 mL 1.2679 mL 2.5358 mL 6.3394 mL
15 mM 0.1691 mL 0.8453 mL 1.6905 mL 4.2263 mL
20 mM 0.1268 mL 0.6339 mL 1.2679 mL 3.1697 mL
25 mM 0.1014 mL 0.5072 mL 1.0143 mL 2.5358 mL
30 mM 0.0845 mL 0.4226 mL 0.8453 mL 2.1131 mL
40 mM 0.0634 mL 0.3170 mL 0.6339 mL 1.5848 mL
50 mM 0.0507 mL 0.2536 mL 0.5072 mL 1.2679 mL
60 mM 0.0423 mL 0.2113 mL 0.4226 mL 1.0566 mL
80 mM 0.0317 mL 0.1585 mL 0.3170 mL 0.7924 mL
100 mM 0.0254 mL 0.1268 mL 0.2536 mL 0.6339 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.

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:
JNJ-7706621
目录号:
HY-10329
需求量: