LY2334737
CAS号 | 892128-60-8 | 货号 | BCP17137 |
中文名 | LY2334737 | ||
英文名 | LY2334737 | ||
中文别名 | |||
英文别名 | LY-2334737;LY 2334737; | ||
分子式 | C17H25F2N3O5 | 分子量 | 389.39 |
生物活性 | in vitro: Five cell lines that express CES2 responded to LY2334737treatment. LY2334737 was less cytotoxic to a SK-OV-3 CES2 knockdown than parental cells. The drug response of CES2-transfected HCT-116 cells correlated with CES2 expression level. Bystander studies showed statistically greater PC-3-GFP growth inhibition by LY2334737 when cells were cocultured with CES2 and not mock transfectants. in vivo: Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once a day for 21 days showed greater tumor growth inhibition of CES2 transfectant than the mock transfectant (P ≤ 0.001) . The MTD was 40 mg LY2334737. Fatigue was the most frequent DLT for LY2334737monotherapy (4 patients) followed by elevated transaminase levels (2 patients), both observed at the 40- to 50-mg dose levels. Among the 10 patients in the combination arm, 2 had DLTs at the 40-mg dose level. These were fatigue and elevated liver enzyme levels. Metronomic LY2334737 administration caused increased blood flow in luci | ||
信号通路 | Cell Cycle/DNA Damage | ||
靶 点 | Antimetabolite |
结构式

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