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.
性状
Solid
体外研究(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 c
体内研究(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
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Zhao H, et al. FL118, a novel anticancer compound, inhibits proliferation and migration of ovarian cancer cells via up-regulation of cytoglobin in vivo and in vitro[J]. Translational Cancer Research, 2017, 6(6):1294-1304.[2]. Ling X, et al. FL118, acting as a molecular glue degrader, binds to dephosphorylates and degrades the oncoprotein DDX5 (p68) to control c-Myc, survivin and mutant Kras against colorectal and pancreatic cancer with high efficacy. Clin Transl Med. 2022 May;12(5):e881.
溶解度数据
In Vitro: DMSO : 2.5 mg/mL (6.37 mM; ultrasonic and warming and heat to 60°C)配制储备液