CK2 inhibitor 2

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CK2 inhibitor 2  纯度: 98.12%

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。

CK2 inhibitor 2

CK2 inhibitor 2 Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
25 mg ￥9500 In-stock
50 mg ￥14500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 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-Akt1S129 and p-Cdc37S13 in HCT-116 cells[1].
CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC50 of 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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-Akt1S129 and p-Cdc37S13 in 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C21H17ClN4O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5456 mL 12.7278 mL 25.4557 mL
5 mM 0.5091 mL 2.5456 mL 5.0911 mL
10 mM 0.2546 mL 1.2728 mL 2.5456 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°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。

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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wang Y, et, al. Discovery of 5-(3-Chlorophenylamino)benzo[ c][2,6]naphthyridine Derivatives as Highly Selective CK2 Inhibitors with Potent Cancer Cell Stemness Inhibition. J Med Chem. 2021 Apr 22;64(8):5082-5098.

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