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JNJ-7706621
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-7706621图片
CAS NO:443797-96-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

JNJ-7706621 is a potentaurora kinaseinhibitor, and also inhibitsCDK1andCDK2, withIC50s of 9 nM, 3 nM, 11 nM, and 15 nM forCDK1,CDK2,aurora-Aandaurora-B, respectively[1][2][3].

IC50& Target

CDK2/cyclinE

3 nM (IC50)

cdk2/cyclin A

4 nM (IC50)

Cdk1/cyclin B

9 nM (IC50)

CDK3/Cyclin E

58 nM (IC50)

CDK6/cyclinD1

175 nM (IC50)

Cdk4/cyclin D1

253 nM (IC50)

Aurora A

11 nM (IC50)

Aurora B

15 nM (IC50)

VEGF-R1

6400 nM (IC50)

VEGF-R2

154 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 shows antiproliferative activity against various human tumor cells with IC50s of 284, 254, and 447 nM for HeLa, HCT116, and A375, respectively[1]. JNJ-7706621 inhibits other centrosomal proteins such as TOG, Nek2, and TACC3 in early mitotic phase, but does not prevent localization of Aurora A to the spindle poles. Treatment of nocodazole-synchronized cells with JNJ-7706621 can override mitotic arrest by preventing spindle checkpoint signaling, resulting in failure of chromosome alignment and segregation[2]. JNJ-7706621 shows inhibition of Aurora-A and Aurora-B but has no activity at the highest concentration tested on the Plk1 or Wee1 serine/threonine kinases. JNJ-7706621 also shows potent growth inhibition in vitro on all human cancer cell types with IC50values ranging from 112 to 514 nM[3]. JNJ-7706621 suspensions inhibits cell viability of HeLa cells with IC50s of 2.1 and 0.9 μg/mL at 24 and 48 h. The IC50of the JNJ-7706621-loaded nanoparticles are 35 and 2.7 μg/mL and the IC50of the JNJ-7706621-loaded micelles are 6.3 and 1.6 μg/mL[4].

体内研究
(In Vivo)

JNJ-7706621 (100 and 125 mg/kg) is efficacious in a human tumor xenograft model under intermittent dosing regimens[3]. JNJ-7706621 (100 mg/kg, i.p.) exhibits 95% tumor growth inhibition in A375 (human melanoma) tumor xenograft model[1]. JNJ-7706621-loaded micelles inhibit tumor growth, and delay the tumor growth more efficiently than the control JNJ-7706621 suspension[4].

分子量

394.36

性状

Solid

Formula

C15H12F2N6O3S

CAS 号

443797-96-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 125 mg/mL(316.97 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5358 mL12.6788 mL25.3575 mL
5 mM0.5072 mL2.5358 mL5.0715 mL
10 mM0.2536 mL1.2679 mL2.5358 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.27 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.27 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 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。

*以上所有助溶剂都可在本网站选购。