中文名 | LY2409881 (trihydrochloride) |
英文名 | LY2409881 (trihydrochloride) |
别名 | LY2409881三盐酸盐 IKK2抑制剂(LY2409881) 化合物LY2409881 TRIHYDROCHLORIDE 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 |
英文别名 | CS-1620 LY2409881 LY2409881 3HCl LY-2409881 HC'l LY2409881 triHCl LY2409881 trihydrochloride LY2409881 (trihydrochloride) 2-(5-chloro-2-(3-(4-methylpiperazin-1-yl)propylamino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide trihydrochloride 2-[5-Chloro-2-[[3-(4-methyl-1-piperazinyl)propyl]amino]-4-pyrimidinyl]-N-cyclopropylbenzo[b]thiophene-4-carboxamide trihydrochloride |
CAS | 946518-60-1 |
化学式 | C24H30Cl2N6OS |
分子量 | 521.51 |
溶解度 | 10毫米DMSO |
存储条件 | -20℃ |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.682 ml | 8.411 ml | 16.823 ml |
5 mM | 0.336 ml | 1.682 ml | 3.365 ml |
10 mM | 0.168 ml | 0.841 ml | 1.682 ml |
5 mM | 0.034 ml | 0.168 ml | 0.336 ml |
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