CK2 inhibitor 2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CK2抑制剂2是一种有效的、选择性的CK2抑制剂(IC50 = 0.66 nM)，具有良好的抗增殖和抗肿瘤活性。

CK2 inhibitor 2 is a potent and selective CK2 inhibitor(IC50 = 0.66 nM) with favorable antiproliferative and antitumor activity.(In Vitro):CK2 inhibitor 2 exhibited stronger CK2 inhibitory activity with higher Clk2/CK2 selectivity(IC50=32.69 nM). 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. CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity (IC50 = 0.10 μM). CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1.(In Vivo):In male BALB/c athymic nude mice, CK2 inhibitor 2 (60-90 mg/kg; p.o. twice a day for 4 weeks) obviously inhibited the tumor growth dose-dependently with a maximum inhibitory rate of 69% at a dose of 90 mg/kg and no conspicuous changes in body weight. In sprague-Dawley (SD) rats, 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).

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-Akt1S129 and p-Cdc37S13 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. 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-Akt1S129 and p-Cdc37S13 in a dose-dependent manner.

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 Cmax (7017.8 ng/mL), elimination half-life (t1/2=6.67 h), and CL (0.60 L/h/kg) in SD rats. 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) ratsDosage: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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Metabolic Enzyme/Protease

Casein Kinase

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2641079-92-5

392.84

C21H17ClN4O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (127.28 mM)

OCCNC(C1=CC(N=C(NC2=CC(Cl)=CC=C2)C3=CC=NC=C34)=C4C=C1)=O

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(-20℃)

With Ice Pack

≥ 2 years