化合物IT-901 T15601

Product Introduction
Bioactivity


英文名: IT-901

描述: IT-901 是一种具有口服活性和有效性的 NF-κB 亚基 c-Rel 抑制剂，对 NF-κB 和 c-Rel 与 DNA 结合的 IC50 分别为 0.1 µM 和 3 μM。IT-901 是一种具有抗肿瘤活性的萘硫代巴比妥酸酯衍生物，可用于预防和治疗人类淋巴瘤和骨髓瘤。

体外活性: Following 24 hours of treatment with IT-901 at concentrations of 1, 3, and 5 μM, there is a reduction in the proliferation of viable ABC and GCB DLBCL cells[2].At a concentration of 3 μM and a duration of 24 hours, IT-901 induces a dose-dependent decrease in cell viability. However, at least 60 percent of cells remain viable after 48 hours of treatment with 4 μM IT-901 in all tested cell lines, except HBL1[2].With a treatment duration of 6 hours and concentrations of 1, 5, and 10 μM, IT-901 leads to a diminished expression of p65 and p50 in both nuclear and cytosolic fractions. Additionally, it reduces the expression of the inhibitory subunit IκBα in both phosphorylated and non-phosphorylated forms in primary CLL cells and cell lines[2].The IC50 of IT-901/GDM-12 is 2.9 μM for c-Rel, while IL-2 secretion is effectively blocked at 5 μM[2].Concentrations of IT-901 above 10 μM become increasingly toxic and may induce apoptosis in healthy cells[2].IT-901 demonstrates inhibition of cell growth in both activated B-like (ABC) and germinal center B-like (GCB) cell lines, with IC50 values ranging between 3 μM to 4 μM[2].

体内活性: Administered intraperitoneally (IP) every other day for 2 weeks at a dose of 24 mg/kg, IT-901 proves to be an effective treatment for acute graft-versus-host disease (GVHD) without compromising its anti-tumor activity[2].IT-901, given at doses ranging from 12 to 20 mg/kg via IP administration, enhances the pharmacokinetic (PK) profile by increasing both half-life (T1/2) and maximum plasma concentration (Cmax)[2].

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

溶解度: DMSO : 10 mg/mL (29.21 mM)


关键字: IT901 | IT-901 | IT 901

相关库: Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途