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| ln Vitro |
The proliferation of ES-2 and SK-O-V3 cells is inhibited by FL118 (0-200 nM; 24, 48, and 72 hours) [1]. The migration of ES-2 and SK-O-V3 cells is inhibited by FL118 (0-100 nM; 0 and 24 hours) [1]. FL118 (0-100 nM; 48 hours) has an impact on cytoglobin (CYGB) expression levels [1]. In ovarian cancer cells, FL118 (10 and 100 nM; 48 h) alters the expression levels of vimentin and E-cadherin and suppresses the PI3K/AKT/mTOR signaling pathway [1]. In 6 and 24 hours, FL118 (0-100 nM) dephosphorylates and breaks down DDX5 [2]. Through control of DDX5, FL118 (0-500 nM; 24, 48, 72 hours) modulates survivin, McL-1, XIAP, cIAP2, c-MYc, and mKras [2]. Significant cytotoxic efficacy against three tumor cell lines (A549, MDA-MB-231, and RM-1 cells) was demonstrated by FL118 (0-1 μM, 24 hours) [3]. FL118 (0–10 nM, 48 hours) causes A549 cells to undergo apoptosis and enhances the synthesis of PARP cleavage [3]. A549 cells are primarily arrested in the G2/M phase by FL118 (0–10 nM, 48 hours) [3].
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| ln Vivo |
FL118 inhibits antitumor activity at doses of 5 and 10 mg/kg, taken once a week for 20 days [1]. Intraperitoneally administered FL118 (0-1.5 mg/kg, five times per diem) efficiently eradicates human colon and head and neck tumors resistant to topotecan or irinotecan [4]. FL118 has good pharmacokinetic properties when given intravenously at a dose of 1.5 mg/kg [4]. Female SCID mice's FL118 pharmacokinetic parameters [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
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: ES-2 and SK-O-V3 cell lines Tested Concentrations: 10 and 100 nM Incubation Duration: 48 h Experimental Results: Effectively inhibited the activation of PI3K/AKT/mTOR signaling pathway in ovarian cancer cells and also inhibited Migration of ES-2 and SK-O-V3 cells. Cell migration assay[1] Cell Types: ES-2 and SK-O-V3 Cell lines Tested Concentrations: 0, 10 and 100 nM Incubation Duration: 0 and 24 hrs (hours) Experimental Results: Inhibition of migrating cells of ES-2 and SK-O-V3 dose dependent. RT-PCR[1] Cell Types: ES-2 and SK-O-V3 cell lines Tested Concentrations: 0, 10 and 100 nM Incubation Duration: 48 hrs (hours) Experimental Results: Promoted CYGB expression. Cell proliferation assay[1] Cell Types: ES-2 and SK-O-V3 Cell lines Tested Concentrations: 0, 1, 10, 50, 100 and 200 nM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Inhibition of ES-2 and SK-O-V3 cells in a time- and dose-dependent manner. Western Blot Analysis[2] Cell Types: SW620 and Mia Paca-2 Tested Concentrations: 0, 10 and 100 nM Incubation Duration: 6 and 24 hrs (hours) Experimental Results: Induced dephosphorylation of DDX5 through the ubiquitin-proteasome degradation pathway and degraded DDX5 time-dependently. Western Blot Analysis[2] Cell Types: PDAC Panc1, CRC HCT-8, SW620, Mia Paca-2, Panc-1, HCT-8 cell lines Tested Concentrations: 0, 10, 100 and 500 nM Incubation Duration: 24, 48, 72 h Experimental Results: 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 Types: A549, MDA-MB-231, RM-1 Tested Concentrations: 0-1 μM Incubation Duration: 24 h Experimental Results: demonstrated 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 Types: A549 cells Tested Concentrations: 0, 2.5, 5, 10 nM Incubation Duration: 48 h Experimental Results: 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 Types: A549 cells Tested Concentrations: 0, 2.5, 5, 10 nM Incubation Duration: 48 h Experimental Results: Increased G2/M cell population in a concentration-dependent manner, and arrested A549 cells mainly at the G2/M phase. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice[1]
Doses: 5 and 10 mg/kg Route of Administration: po (oral gavage); 5 mg/kg once weekly; 10 mg/kg once weekly; 20-day Experimental Results: demonstrated Bitot Potecan has better anti-tumor activity and dose-dependently inhibits the growth of ES-2 tumors by upregulating the expression level of CYGB. Animal/Disease Models: SCID (severe combined immunodeficiency) mice (ten weeks old, female, 20-25 g, 5 mice per cage) bearing human SW620 (colon) and FaDu (head and neck) xenograft tumors [4]: 0, 0.75, 1, 1.5 mg/kg Doses: IP, once every other day, five times as one cycle (if the tumor relapses, mice are treated with FL118 for the second or third cycle) Experimental Results: Elimination and acquisition of iritinib can detect human xenograft tumors or topotecan resistance and was effective after multiple cycles of treatment without developing FL118 resistance. Animal/Disease Models: SCID (severe combined immunodeficiency) mice harboring human SW620 (colon) and FaDu SCID (severe combined immunodeficient) mouse harboring human SW620 (colon) and FaDu (h |
| References |
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| Molecular Formula |
C21H16N2O6
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|---|---|
| Molecular Weight |
392.36200
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| Exact Mass |
392.101
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| CAS # |
135415-73-5
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| Related CAS # |
(R)-FL118;151636-76-9
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| PubChem CID |
72403
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| Appearance |
Light brown to brown solid powder
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| Density |
1.64g/cm3
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| Boiling Point |
812.1ºC at 760mmHg
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| Flash Point |
445ºC
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| LogP |
1.808
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
29
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| Complexity |
852
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=C6C(=CC5=C4)OCO6)O
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| InChi Key |
RPFYDENHBPRCTN-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C21H16N2O6/c1-2-21(26)13-5-15-18-11(7-23(15)19(24)12(13)8-27-20(21)25)3-10-4-16-17(29-9-28-16)6-14(10)22-18/h3-6,26H,2,7-9H2,1H3/t21-/m0/s1
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| Chemical Name |
(5S)-5-ethyl-5-hydroxy-7,18,20-trioxa-11,24-diazahexacyclo[11.11.0.02,11.04,9.015,23.017,21]tetracosa-1(13),2,4(9),14,16,21,23-heptaene-6,10-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~1 mg/mL (~2.55 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5487 mL | 12.7434 mL | 25.4868 mL | |
| 5 mM | 0.5097 mL | 2.5487 mL | 5.0974 mL | |
| 10 mM | 0.2549 mL | 1.2743 mL | 2.5487 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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