CK2 inhibitor 2 (C09-1121-024)

CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2 , with an IC 50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC 50 =32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activityIn VitroCK2 inhibitor 2 (compound 1c) exhibits potent antiproliferative activities against PC-3, HCT-116, MCF-7, HT-29, T24 and LO2 cells, with IC 50 s 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 IC 50 of 0.10 μM. CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1 in HCT-116 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell 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 AnalysisCell 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.In VivoCK2 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 . MCE 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.Form:SolidIC50& Target:CK2 0.66 nM (IC 50 ). Specifications and Purity: 98%. Molecular Formula: C21H17ClN4O2. Molecular Weight: 392.84.