FL118
Based on 3 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.22%
- CAS No.: 135415-73-5
- Formula: C21H16N2O6
- Molecular Weight:392.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) FL118
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Biological Activity
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Cell Line
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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 | EC50 |
0.86 nM
Compound: 11; FL118
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
|
[PMID: 38421819] |
| A549 | IC50 |
0.009 μM
Compound: 3; FL118
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 38092421] |
| 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] |
| A549 | IC50 |
43 ng/mL
Compound: 11; FL118
|
Cytotoxicity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 38421819] |
| A549 | IC50 |
50.7 nM
Compound: FL118
|
Growth inhibition of human A549 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
Growth inhibition of human A549 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
|
[PMID: 38100041] |
| 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] |
| EKVX | IC50 |
0.006 μM
Compound: 3; FL118
|
Antiproliferative activity against human EKVX cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human EKVX cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 38092421] |
| 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] |
| HCT-116 | EC50 |
0.36 nM
Compound: 11; FL118
|
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
|
[PMID: 38421819] |
| HCT-116 | IC50 |
0.005 μM
Compound: 3; FL118
|
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 38092421] |
| HCT-116 | IC50 |
23.5 nM
Compound: FL118
|
Growth inhibition of human HCT-116 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
Growth inhibition of human HCT-116 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
|
[PMID: 38100041] |
| HCT-116 | IC50 |
50 ng/mL
Compound: 11; FL118
|
Cytotoxicity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 38421819] |
| HCT-8 | IC50 |
0.005 μM
Compound: 3; FL118
|
Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth
Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth
|
[PMID: 38092421] |
| HeLa | IC50 |
32.4 nM
Compound: FL118
|
Growth inhibition of human HeLa cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
Growth inhibition of human HeLa cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
|
[PMID: 38100041] |
| HeLa | IC50 |
40 ng/mL
Compound: 11; FL118
|
Cytotoxicity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 38421819] |
| HeLa | IC50 |
9.6 nM
Compound: Methylenedioxy Camptothecin (table 1)
|
Concentration required to inhibit growth of human cervical HeLa carcinoma cell line
Concentration required to inhibit growth of human cervical HeLa carcinoma cell line
|
[PMID: 15454230] |
| 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] |
| HepG2 | IC50 |
104 ng/mL
Compound: 11; FL118
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 38421819] |
| HepG2 | IC50 |
39.5 nM
Compound: FL118
|
Growth inhibition of human HepG2 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
Growth inhibition of human HepG2 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
|
[PMID: 38100041] |
| 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 |
32.2 nM
Compound: FL118
|
Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT reagent based ELISA reader analysis
|
[PMID: 38100041] |
| 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-H460 | IC50 |
0.003 μM
Compound: 3; FL118
|
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 38092421] |
| 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] |
| NSCLC | EC50 |
1 nM
Compound: 24; FL118, Table 2, cpd 7
|
Cytotoxicity against human NSCLC cells
Cytotoxicity against human NSCLC cells
|
[PMID: 34175539] |
| PC-3 | IC50 |
8.1 nM
Compound: Methylenedioxy Camptothecin (table 1)
|
Concentration required to inhibit growth of human prostate PC-3 carcinoma cell line
Concentration required to inhibit growth of human prostate PC-3 carcinoma cell line
|
[PMID: 15454230] |
| 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 |
0.009 μM
Compound: 3; FL118
|
Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 38092421] |
| 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] |
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.
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Cell Line:ES-2 and SK-O-V3 cell lines
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Concentration:10 and 100 nM
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Incubation Time:48 h
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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.
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Cell Line:ES-2 and SK-O-V3 cell lines
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Concentration:0, 10 and 100 nM
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Incubation Time:0 and 24 h
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Result:Inhibited the migration of ES-2 and SK-O-V3 cells dose-dependenly.
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Cell Line:ES-2 and SK-O-V3 cell lines
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Concentration:0, 10 and 100 nM
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Incubation Time:48 h
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Result:Promoted CYGB expression.
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Cell Line:ES-2 and SK-O-V3 cell lines
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Concentration:0, 1, 10, 50, 100 and 200 nM
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Incubation Time:24, 48 and 72 h
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Result:Inhibited the cell proliferation of ES-2 and SK-O-V3 cells time- and dose-dependently.
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Cell Line:SW620 and Mia Paca-2
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Concentration:0, 10 and 100 nM
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Incubation Time:6 and 24 h
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Result:Induced dephosphorylation of DDX5 through the ubiquitin-proteasome degradation pathway and degraded DDX5 time-dependently.
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Cell Line:PDAC Panc1, CRC HCT-8, SW620, Mia Paca-2, Panc-1, HCT-8 cell lines
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Concentration:0, 10, 100 and 500 nM
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Incubation Time:24, 48, 72 h
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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.
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Cell Line:A549, MDA-MB-231, RM-1
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Concentration:0-1 μM
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Incubation Time:24 h
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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.
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Cell Line:A549 cells
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Concentration:0, 2.5, 5, 10 nM
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Incubation Time:48 h
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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.
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Cell Line:A549 cells
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Concentration:0, 2.5, 5, 10 nM
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Incubation Time:48 h
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Result:Increased G2/M cell population in a concentration-dependent manner, and arrested A549 cells mainly at the G2/M phase.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fmale BALB/c nude mice[1]
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Dosage:5 and 10 mg/kg
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Administration:Oral gavage; 5 mg/kg for once a week; 10 mg/kg for once a week; for 20 days
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Result:Showed better antitumor activity than topotecan and dose-dependenly suppressed the growth of ES-2 tumors by upregulating the expression level of CYGB.
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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]
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Dosage:0, 0.75, 1, 1.5 mg/kg
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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)
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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.
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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]
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Dosage:1.5 mg/kg
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Administration:IV, once
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Result:Exhibited favorable pharmacokinetics profiles.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 135415-73-5
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Appearance Solid
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Molecular Weight 392.36
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Formula C21H16N2O6
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Color Light brown to brown
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SMILES
O=C1[C@](O)(CC)C(C=C2C3=NC4=CC5=C(C=C4C=C3CN2C6=O)OCO5)=C6CO1
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Synonyms
10,11-(Methylenedioxy)-20(S)-camptothecin
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
-
Most Recent
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Int Immunopharmacol
Targeting DDX5 using FL118 suppresses mTOR signaling and tumorigenicity in JAK2V617F-driven myeloproliferative neoplasms. [Abstract]2026 Jan 31:173:116284. PMID: 41621382 -
Cell Signal
USP7-DDX5-FASN axis drives fatty acid metabolism and supports hepatocellular carcinoma progression. [Abstract]2025 Jun 17:111947. PMID: 40553965 -
Solvent & Solubility
DMSO : 1 mg/mL (2.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (292 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Portuguese - PT (420 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5487 mL | 12.7434 mL | 25.4868 mL | 63.7170 mL |