化合物CK2 inhibitor 2 T35557

Product Introduction
Bioactivity


英文名: CK2 inhibitor 2

描述: CK2 inhibitor 2 是一种有效的，选择性和口服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 表现出良好的抗增殖和抗肿瘤活性。

体外活性: CK2 inhibitor 2 (compound 1c) exhibits effective 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 [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-Akt1 S129 and p-Cdc37 S13 in HCT-116 cells [1]. CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC 50 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]. 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-Akt1 S129 and p-Cdc37 S13 in a dose-dependent manner.

体内活性: CK2 inhibitor 2 (60-90 mg/kg; p.o. twice a day for 4 weeks) significantly 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 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 [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: C max =7017.8 ng/mL, t 1/2 =6.67 h, CL=0.60 L/h/kg.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (127.28 mM)


关键字: CK-2 inhibitor 2 | CK2 inhibitor 2

相关产品: PF-4800567 | Casein kinase 1δ-IN-6 | CK2-IN-4 | PF-5006739 | Casein kinase 1δ-IN-4 | Emodin | DMAT | TAK-715 | CX-5011 | BMS-863233 HCl

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | Bioactive Compound Library

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