2. Apoptosis
  3. Survivin Apoptosis IAP
  4. FL118

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

Cat. No.: HY-12486 Purity: 99.14%
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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.

FL118 Chemical Structure

FL118 Chemical Structure

CAS No. : 135415-73-5

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Based on 1 publication(s) in Google Scholar

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FL118 Related Antibodies

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cIAP cIAP-1 cIAP-2 XIAP

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Description

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].

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].

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

FL118 Related Antibodies

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.
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

MedChemExpress (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.
Molecular Weight

392.36

Formula

C21H16N2O6
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

O=C1[C@](O)(CC)C(C=C2C3=NC4=CC5=C(C=C4C=C3CN2C6=O)OCO5)=C6CO1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5487 mL 12.7434 mL 25.4868 mL
5 mM --- --- ---
View the 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.

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Purity & Documentation

Purity: 99.14%

COA (256 KB) HNMR (422 KB) RP-HPLC (1609 KB)

Handling Instructions (2659 KB)
References

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
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FL118 Related Classifications

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.

Keywords:

FL118135415-73-510,11-(Methylenedioxy)-20(S)-camptothecinFL 118FL-118SurvivinApoptosisIAPcamptothecin analoguegrowthmetastasisproliferationmigrationpyroptosisA549 cellMDA-MB-231RM-1Inhibitorinhibitorinhibit

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