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FL118
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FL118图片
CAS NO:135415-73-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
10,11-(Methylenedioxy)-20(S)-camptothecin
产品介绍
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), aCamptothecin(HY-16560) analogue, is a potent and orally activesurvivininhibitor. FL118 binds to oncoproteinDDX5 (p68)to dephosphorylates and degrades DDX5. FL118 can be used for the research ofcancer[1][2].

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-V3cells[1].
FL118 (0-100 nM; 0 and 24 h) inhibits the migration of ES-2 and SK-O-V3cells[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].

Western Blot Analysis[1]

Cell Line:ES-2 and SK-O-V3cell lines
Concentration:10 and 100 nM
Incubation Time:48 h
Result:Effectively inhibited the activation of PI3K/AKT/mTOR signaling pathway in ovarian cancer cells and also inhibited the migration of ES-2 and SK-O-V3cells.

Cell Migration Assay[1]

Cell Line:ES-2 and SK-O-V3cell lines
Concentration:0, 10 and 100 nM
Incubation Time:0 and 24 h
Result:Inhibited the migration of ES-2 and SK-O-V3cells dose-dependenly.

RT-PCR[1]

Cell Line:ES-2 and SK-O-V3cell lines
Concentration:0, 10 and 100 nM
Incubation Time:48 h
Result:Promoted CYGB expression.

Cell Proliferation Assay[1]

Cell Line:ES-2 and SK-O-V3cell lines
Concentration:0, 1, 10, 50, 100 and 200 nM
Incubation Time:24, 48 and 72 h
Result:Inhibited the cell proliferation of ES-2 and SK-O-V3cells time- and dose-dependently.

Western Blot Analysis[2]

Cell Line:SW620 and Mia Paca-2
Concentration:0, 10 and 100 nM
Incubation Time:6 and 24 h
Result:Induced dephosphorylation of DDX5 through the ubiquitin-proteasome degradation pathway and degraded DDX5 time-dependently.

Western Blot Analysis[2]

Cell Line:PDAC Panc1, CRC HCT-8, SW620, Mia Paca-2, Panc-1, HCT-8 cell lines
Concentration:0, 10, 100 and 500 nM
Incubation Time:24, 48, 72 h
Result:Controled the expression of survivin, Mcl-1, XIAP, cIAP2, c-Myc and mKras by regulated DDX5, as an upstream master regulator in cancer development and malignant networks.

Cell Cytotoxicity Assay[3]

Cell Line:A549, MDA-MB-231, RM-1
Concentration:0-1 μM
Incubation Time:24 h
Result:Showed cytotoxicity in A-549 (human lung carcinoma), MDA-MB-231 (human breast carcinoma) and RM-1 (mouse prostate carcinoma), with IC50values of 8.94 ± 1.54 , 24.73 ± 13.82, and 69.19 ± 8.34 nM, respectively.

Apoptosis Analysis[3]

Cell Line:A549 cells
Concentration:0, 2.5, 5, 10 nM
Incubation Time:48 h
Result:Resulted in the downregulation of survivin. Increased the production of PARP cleavage in a concentration-dependent manner, which is the hallmark of apoptosis. Induced apoptosis in A549.

Cell Cycle Analysis[3]

Cell Line:A549 cells
Concentration:0, 2.5, 5, 10 nM
Incubation Time:48 h
Result:Increased G2/M cell population in a concentration-dependent manner, and arrested A549 cells mainly at the G2/M phase.
体内研究
(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].

SampleFaDuSW620Plasma
T1/2(hr)6.85212.751.788
Tmax(hr)0.1670.1670.167
Cmax(ng/g, mL)11515843
AUC (hr*ng/g)41384282
AUC(hr*ng/g)448897104
AUC% Extrap (%)7.746.1721.7
Vz (g/kg) (ml/kg)330523074236849
Cl (g/hr/kg) (ml/hr/kg)3343167114287

Animal Model:Fmale BALB/c nude mice[1]
Dosage:5 and 10 mg/kg
Administration:Oral gavage; 5 mg/kg for once a week; 10 mg/kg for once a week; for 20 days
Result:Showed better antitumor activity than topotecan and dose-dependenly suppressed the growth of ES-2 tumors by upregulating the expression level of CYGB.
Animal Model:SCID (severe combined immunodeficiency) mice bearing human SW620 (colon) and FaDu (head-and-neck) xenograft tumors (ten-week-old, female, 20-25 g, 5 mice per cage)[4]
Dosage:0, 0.75, 1, 1.5 mg/kg
Administration:IP, once every other day for five times as one cycle (If tumors relapse, mice were treated with FL118 for second or third cycles)
Result:Eliminated human xenograft tumors that acquired irinotecan or topotecan resistance, and was also effective after multiple cycles of treatment without the generation of FL118 resistance.
Animal Model:SCID (severe combined immunodeficiency) mice bearing human SW620 (colon) and FaDu SCID mice bearing human SW620 (colon) and FaDu (head-and-neck) xenograft tumors (ten-week-old, female, 20-25 g, 5 mice per cage)[4]
Dosage:1.5 mg/kg
Administration:IV, once
Result:Exhibited favorable pharmacokinetics profiles.
分子量

392.36

性状

Solid

Formula

C21H16N2O6

CAS 号

135415-73-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 2.5 mg/mL(6.37 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5487 mL12.7434 mL25.4868 mL
5 mM0.5097 mL2.5487 mL5.0974 mL
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。