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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) dephosphorylates and degrades 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 and 10 mg/kg; p.o. once a week for 20 days) inhibits antitumor activity.
FL118 (0-1.5 mg/kg, i.p. 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, i.v. once) exhibits favorable pharmacokinetics profiles.
Pharmacokinetic Parameters of FL118 in female SCID mice.
Sample | FaDu | SW620 | Plasma |
T1/2 (hr) | 6.852 | 12.75 | 1.788 |
Tmax (hr) | 0.167 | 0.167 | 0.167 |
Cmax (ng/g, mL) | 115 | 158 | 43 |
AUC (hr*ng/g) | 413 | 842 | 82 |
AUC∞ (hr*ng/g) | 448 | 897 | 104 |
AUC% Extrap (%) | 7.74 | 6.17 | 21.7 |
Vz (g/kg) (ml/kg) | 33052 | 30742 | 36849 |
Cl (g/hr/kg) (ml/hr/kg) | 3343 | 1671 | 14287 |
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货号: HY-12486
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