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CK2 inhibitor 2
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。
CK2 inhibitor 2图片
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
CK2 inhibitor 2 是一种有效的,选择性和具有口服活性的CK2抑制剂,IC50值为 0.66 nM。CK2 inhibitor 2 对 Clk2 (IC50=32.69 nM)/CK2 显示出高选择性。 CK2 inhibitor 2 具有良好的抗增殖和抗肿瘤活性。
生物活性

CK2 inhibitor2 is a potent, selective and orally active inhibitor ofCK2, with anIC50of 0.66 nM.CK2 inhibitor2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2.CK2 inhibitor2 exhibits favorable antiproliferative and antitumor activity[1].

IC50& Target[1]

CK2

0.66 nM (IC50)

体外研究
(In Vitro)

CK2 inhibitor 2 (compound 1c) exhibits potent antiproliferative activities against PC-3, HCT-116, MCF-7, HT-29, T24 and LO2 cells, with IC50s of 4.53 μM, 3.07 μM, 7.50 μM, 5.18 μM, 6.10 μM, and 96.68 μM, respectively[1].
CK2 inhibitor 2 (5-20 μM; 24 h) induces apoptosis of HCT-116 cells in a dose-dependent manner. CK2 inhibitor 2 dose-dependently suppresses the expression of p-Akt1S129and p-Cdc37S13in HCT-116 cells[1].
CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC50of 0.10 μM[1].
CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1 in HCT-116 cells[1].

Apoptosis Analysis[1]

Cell Line:HCT-116 cells
Concentration:5, 10, 20 μM
Incubation Time:24 hours
Result:The apoptotic ratio reached about 55% at the concentration of 20 μM.

Western Blot Analysis[1]

Cell Line:HCT-116 cells
Concentration:5, 10, 20 μM
Incubation Time:24 hours
Result:Inhibited the expression of p-Akt1S129and p-Cdc37S13in a dose-dependent manner.
体内研究
(In Vivo)

CK2 inhibitor 2 (60-90 mg/kg; p.o. twice a day for 4 weeks) obviously inhibits the tumor growth dose-dependently with a maximum inhibitory rate of 69% at a dose of 90 mg/kg[1].
CK2 inhibitor 2 (25 mg/kg; a single p.o.) exhibits Cmax(7017.8 ng/mL), elimination half-life (t1/2=6.67 h), and CL (0.60 L/h/kg) in SD rats[1].

Animal Model:Male BALB/c athymic nude mice (5 weeks old; 16-18 g) were injected HCT-116 cells[1]
Dosage:60, 90 mg/kg
Administration:P.o. twice a day for 4 weeks
Result:Inhibited the tumor growth in a dose-dependent manner.
No conspicuous change in body weight.
Animal Model:Sprague-Dawley (SD) rats[1]
Dosage:25 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:Cmax=7017.8 ng/mL, t1/2=6.67 h, CL=0.60 L/h/kg.
分子量

392.84

性状

Solid

Formula

C21H17ClN4O2

运输条件

Room temperature in continental US; may vary elsewhere.

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

DMSO : 50 mg/mL(127.28 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5456 mL12.7278 mL25.4557 mL
5 mM0.5091 mL2.5456 mL5.0911 mL
10 mM0.2546 mL1.2728 mL2.5456 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    90%corn oil

    Solubility: 2.08 mg/mL (5.29 mM); Clear solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.29 mM) 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。