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发布者：信康 浏览次数：
产品名称:N/ACAS:946518-60-1别名：2-[5-氯-2-[[3-(4-甲基-1-哌嗪基)丙基]氨基]-4-嘧啶基]-N-环丙基-苯并[B]噻吩-4-甲酰胺三盐酸盐英文名：LY2409881 trihydrochloride
[] - 生物活性LY2409881 是一种有效的选择性 IKK2 抑制剂，IC50 为 30 nM，选择性比IKK1和其他常见激酶高10倍多。
- 体外研究LY2409881 inhibits constitutively activated NF-ƘB, and causes concentration- and time-dependent growth inhibition and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity. LY2409881 is synergistic with doxorubicin and cyclophosphamide in SUDHL2 cell in inhibiting the cell growth, but not in LY1 cell. In both SUDHL2 and LY1 cells, LY2409881 is synergistic with the histone deacetylase (HDAC) inhibitor romidepsin in inhibiting the cell growth.
- 体内研究In SCID-beige xenograft mouse model, LY2409881 (50, 100, and 200 mg/kg, i.p.) significantly inhibits the tumor growth.
