CK2 inhibitor 2|cas:2641079-92-5|西域试剂

CK2 inhibitor 2,98.12%

产品编号：Bellancom-132175| CAS NO：2641079-92-5| 分子式：C₂₁H₁₇ClN₄O₂| 分子量：392.84

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货号	价格	库存与货期
Bellancom-132175	￥3000.00	杭州北京（现货）
Bellancom-132175	￥4800.00	杭州北京（现货）
Bellancom-132175	￥9500.00	杭州北京（现货）
Bellancom-132175	￥14500.00	杭州北京（现货）
Bellancom-132175	￥22500.00	杭州北京（现货）

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CK2 inhibitor 2

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 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.

体外研究

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.
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-Akt1^S129 and p-Cdc37^S13 in HCT-116 cells.
CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC₅₀ of 0.10 μM.
CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1 in HCT-116 cells.

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

Apoptosis Analysis

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

Cell Line:	HCT-116 cells
Concentration:	5, 10, 20 μM
Incubation Time:	24 hours
Result:	Inhibited the expression of p-Akt1^S129 and p-Cdc37^S13 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.
CK2 inhibitor 2 (25 mg/kg; a single p.o.) exhibits C_max (7017.8 ng/mL), elimination half-life (t_1/2=6.67 h), and CL (0.60 L/h/kg) in SD rats.

西域 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
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
Dosage:	25 mg/kg (Pharmacokinetic Analysis)
Administration:	A single p.o.
Result:	C_max=7017.8 ng/mL, t_1/2=6.67 h, CL=0.60 L/h/kg.

体内研究

西域 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
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
Dosage:	25 mg/kg (Pharmacokinetic Analysis)
Administration:	A single p.o.
Result:	C_max=7017.8 ng/mL, t_1/2=6.67 h, CL=0.60 L/h/kg.

体内研究

西域 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
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
Dosage:	25 mg/kg (Pharmacokinetic Analysis)
Administration:	A single p.o.
Result:	C_max=7017.8 ng/mL, t_1/2=6.67 h, CL=0.60 L/h/kg.

性状

Solid

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。