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] | |
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. |
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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. |
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| 分子量 | |
| 性状 | |
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| 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 |
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| 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 | 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℃, 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。 |
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