| 中文名称 |
FL118
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| 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
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| 英文名称 |
FL118
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| 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
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| Cas No. |
135415-73-5
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| 分子式 |
C21H16N2O6
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| 分子量 |
392.36
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| 包装储存 |
Powder -20°C 3 years;4°C 2 years
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| 详情描述 |
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。
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| 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。
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| 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.
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| 性状 |
Solid
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| 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
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| 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
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| 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.
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| 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]. 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.
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。