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  2. Apoptosis
  3. Survivin Apoptosis IAP
  4. FL118

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

目錄號: HY-12486 純度: 99.40%
COA 產(chǎn)品使用指南 技術(shù)支持

FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin)，一種喜樹堿 (Camptothecin; HY-16560) 類似物，是一種口服有效的 survivin 抑制劑。FL118 與 DDX5 (p68) 結(jié)合，去磷酸化并降解 DDX5。FL118 可用于癌癥的研究。

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FL118 Chemical Structure

FL118 Chemical Structure

CAS No. : 135415-73-5

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1 mg ￥450
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5 mg ￥900
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25 mg ￥2300
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50 mg ￥4200
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查看 IAP 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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[1][2].

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
2008 IC50
37.28 nM
Compound: 4; FL118
Antiproliferative activity against human 2008 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human 2008 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
A549 IC50
0.083 μM
Compound: 24; FL118, Table 2, cpd 7
Cytotoxicity against human A549 cells incubated for 48 hrs by by SpectraMax M5 microplate reader analysis
Cytotoxicity against human A549 cells incubated for 48 hrs by by SpectraMax M5 microplate reader analysis
[PMID: 34175539]
Bel-7402 IC50
21.75 nM
Compound: 4; FL118
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
H69AR IC50
6.29 nM
Compound: 4; FL118
Antiproliferative activity against human NCI-H69AR cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human NCI-H69AR cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
HepG2 IC50
10.64 nM
Compound: 4; FL118
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
HL-60 IC50
0.027 μM
Compound: 5z
Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells
Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells
[PMID: 8410981]
MCF7 IC50
63.26 nM
Compound: 4; FL118
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
NCI-H446 IC50
18.54 nM
Compound: 4; FL118
Antiproliferative activity against Irinotecan-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against Irinotecan-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
NCI-H446 IC50
6.61 nM
Compound: 4; FL118
Antiproliferative activity against etoposide/cisplatin combination-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against etoposide/cisplatin combination-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
NCI-H446 IC50
8.87 nM
Compound: 4; FL118
Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
NCI-H69 IC50
15.81 nM
Compound: 4; FL118
Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
SH-SY5Y IC50
24.19 nM
Compound: 4; FL118
Antiproliferative activity against human SH-SY5Y cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human SH-SY5Y cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
SW-620 IC50
0.93 nM
Compound: 4; FL118
Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
U-87MG ATCC IC50
108.57 nM
Compound: 4; FL118
Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
[PMID: 35932565]
體外研究
(In Vitro)

FL118 (0-200 nM; 24, 48 and 72 h ) inhibits the cell proliferation of ES-2 and SK-O-V3 cells[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].

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

Western Blot Analysis[1]

Cell Line: ES-2 and SK-O-V3 cell 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-V3 cells.

Cell Migration Assay [1]

Cell Line: ES-2 and SK-O-V3 cell lines
Concentration: 0, 10 and 100 nM
Incubation Time: 0 and 24 h
Result: Inhibited the migration of ES-2 and SK-O-V3 cells dose-dependenly.

RT-PCR[1]

Cell Line: ES-2 and SK-O-V3 cell 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-V3 cell 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-V3 cells 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 IC50 values 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.
體內(nèi)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].

Sample FaDu SW620 Plasma
T1/2 (hr) 6.852 12.75 1.788
Tmax (hr) 0.167 0.167 0.167
Cmax (ng/g, mL) 115 158 43
AUC (hr*ng/g) 413 842 82
AUC∞ (hr*ng/g) 448 897 104
AUC% Extrap (%) 7.74 6.17 21.7
Vz (g/kg) (ml/kg) 33052 30742 36849
Cl (g/hr/kg) (ml/hr/kg) 3343 1671 14287

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

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

Formula

C21H16N2O6
CAS 號
性狀

固體

顏色

Light brown to brown

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 1 mg/mL (2.55 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5487 mL 12.7434 mL 25.4868 mL
5 mM --- --- ---
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* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

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動物數(shù)量

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由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.40%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5487 mL 12.7434 mL 25.4868 mL 63.7170 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
FL118
目錄號：
HY-12486
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