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FL118

CAS No. : 135415⁻⁷3-5

MCE 国际站：FL118

产品活性：FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin)，一种喜树碱 (Camptothecin; HY-16560) 类似物，是一种口服有效的 survivin 抑制剂。FL118 与 DDX5 (p68) 结合，去磷酸化并降解 DDX5。FL118 可用于癌症的研究。

研究领域：Apoptosis

作用靶点：Survivin | Apoptosis | IAP

In Vitro: FL118 (0-200 nM; 24, 48 ａnd 72 h ) inhibits the cell proliferation of ES-2 ａnd SK-O-V₃ cells.
FL118 (0-100 nM; 0 ａnd 24 h) inhibits the migration of ES-2 ａnd SK-O-V₃ cells.
FL118 (0-100 nM; 48 h) affects the expression level of cytoglobin (CYGB).
FL118 (10 ａnd 100 nM; 48 h) inhibits PI3K/AKT/mTOR signaling pathway, ａnd affects the expression level of vimentin ａnd E-cadherin in ovarian cancer cells.
FL118 (0-100 nM; 6 ａnd 24 h) can dephosphorylate ａnd degrade DDX5.
FL118 (0-500 nM; 24, 48, 72 h) regulates survivin, McL-1, XIAP, cIAP2, c-MYc ａnd mKras by regulating DDX5.
FL118 (0-1 µM, 24 h) shows significant cytotoxic activity against the three tumor cell lines (A549, MDA-MB-231, ａnd RM-1 cells).
FL118 (0-10 nM, 48 h) increases the production of PARP cleavage, ａnd induces apoptosis in A549.
FL118 (0-10 nM, 48 h) arrests A549 cells mainly at the G2/M phase.

In Vivo: FL118 (5, 10 mg/kg; p.o. once a week; for 20 days) inhibits antitumor activity.
FL118 (0-1.5 mg/kg, IP, once every other day for five times) effectively eliminates human colon ａnd head-and-neck tumors that acquire irinotecan or topotecan resistance.
FL118 (1.5 mg/kg, IV, once) exhibits favorable pharmacokinetics (PK) profiles.

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