FL118 (Synonyms: 10,11-(Methylenedioxy)-20(S)-camptothecin)
目录号: PL02716 纯度: ≥97%
CAS No. :135415-73-5
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中文名称
FL118
中文别名
(7S)-7-乙基-7-羟基-10H-1,3-二氧杂环[4,5-g]吡拉诺[3',4':6,7]吲哚并[1,2-b]喹啉-8,11(7H,13H)-二酮
英文名称
FL118
英文别名
(7S)-7-ethyl-7-hydroxy-10H-1,3-Dioxolo[4,5-g]pyrano[3',4':6,7]indolizino[1,2-b]quinoline-8,11(7H,13H)-dione;10,11-methylenedioxycamptothecin;Mdo-cpt;compound 5z [PMID: 8410981];NSC634724;10,11-CH2O2-Camptothecin;GTPL8893;10,11-Methylenedioxy-camptothecin;10,11-Methylenedioxy-20S-camptothecin;FL118
Cas No.
135415-73-5
分子式
C21H16N2O6
分子量
392.36
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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