FL118  (Synonyms: 10,11-(Methylenedioxy)-20(S)-camptothecin)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

392.36

C₂₁H₁₆N₂O₆

135415-73-5

Solid

Light brown to brown

O=C1[C@](O)(CC)C(C=C2C3=NC4=CC5=C(C=C4C=C3CN2C6=O)OCO5)=C6CO1

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [3]. Wu G, et al. Synthesis of novel 10,11-methylenedioxy-camptothecin glycoside derivatives and investigation of their anti-tumor effects in vivo. RSC Adv. 2019 Apr 9;9(20):11142-11150.  [Content Brief]

  [4]. Ling X, et, al. FL118, a novel camptothecin analogue, overcomes irinotecan and topotecan resistance in human tumor xenograft models. Am J Transl Res. 2015 Oct 15;7(10):1765-81.  [Content Brief]