FL118

FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer^[1][2]. In Vitro: FL118 (0-200 nM; 24, 48 and 72 h ) inhibits the cell proliferation of ES-2 and SK-O-V₃ cells^[1].
FL118 (0-100 nM; 0 and 24 h) inhibits the migration of ES-2 and SK-O-V₃ cells^[1].
FL118 (0-100 nM; 48 h) affects the expression level of cytoglobin (CYGB)^[1].
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^[1].
FL118 (0-100 nM; 6 and 24 h) dephosphorylates and degrades DDX5^[2].
FL118 (0-500 nM; 24, 48, 72 h) regulates survivin, McL-1, XIAP, cIAP2, c-MYc and mKras by regulating DDX5^[2].
FL118 (0-1 μM, 24 h) shows significant cytotoxic activity against the three tumor cell lines (A549, MDA-MB-231, and RM-1 cells)^[3].
FL118 (0-10 nM, 48 h) increases the production of PARP cleavage, and induces apoptosis in A549^[3].
FL118 (0-10 nM, 48 h) arrests A549 cells mainly at the G2/M phase^[3]. In Vivo: FL118 (5 and 10 mg/kg; p.o. once a week for 20 days) inhibits antitumor activity^[1].
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^[4].
FL118 (1.5 mg/kg, i.v. once) exhibits favorable pharmacokinetics profiles^[4].
Pharmacokinetic Parameters of FL118 in female SCID mice^[4].

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