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Purity: ≥98%
EL102, a novel toluidine sulphonamide, is a novel inhibitor of HIF1α (hypoxia inducible factor) and can also potently inhibit tubulin polymerisation and decreased microtubule stability. EL102 has in vitro activity against prostate cancer, characterised by accumulation in G2/M, induction of apoptosis, inhibition of Hif1α, and inhibition of tubulin polymerisation and decreased microtubule stability. In vivo, a combination of EL102 and docetaxel exhibits superior tumour inhibition. The DLKP cell line and multidrug-resistant DLKPA variant (which exhibits 205 to 691-fold greater resistance to docetaxel, paclitaxel, vincristine and doxorubicin) are equally sensitive to EL102. In conclusion, EL102 shows potential as both a single agent and within combination regimens for the treatment of prostate cancer, particularly in the chemoresistance setting.
| ln Vitro |
In vitro growth of prostate cancer cells is inhibited by EL-102 (0-120 nM; 72 hours) [1]. Prostate cancer cell lines are cytotoxic to EL-102 (0-100 nM; 72 hours) [1]. EL-102 (10-100 nM; 24-72 hours) alters the cell cycle and causes apoptosis [1]. In DU145 cells, EL-102 (10–100 nM; 24-48 hours) influences PARP cleavage [1]. Inhibiting tubulin polymerization activity, EL-102 (5 nM; 0-60 min) [1]. Hif1α protein expression is inhibited by EL-102 (0-100 nM; 1 hour) [1].
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| ln Vivo |
The in vivo effects of docetaxel are enhanced by EL-102 (12 and 15 mg/kg; administered orally for 5 days, with 2 days off, 13 to 37 days following tumor transplantation) [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA Cell Line Tested Concentrations: 0-120 nM Incubation Duration: 72 hrs (hours) Experimental Results: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA The IC50 of mycin-selected variant DLKPA cells were 24, 21.7, 40.3, 37.0, 14.4 and 16.3 nM, respectively. Cytotoxicity assay[1] Cell Types: CWR22, 22Rv1, DU145 and PC-3 cell lines Tested Concentrations: 0-100 nM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated cytotoxicity to prostate cancer cell lines and inhibited prostate cancer cell lines No additive effects on cell viability of docetaxel. Apoptosis analysis[1] Cell Types: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA Cell line Tested Concentrations: 10 and 100 nM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Induction of apoptosis with a certain dose, Inhibits cell viability 100 nm. Western Blot Analysis [1] Cell Types: DU145 Cell line Tested Concentrations: 10 and 100 nM Incubation Duration: 24 and 48 hrs (hours) Experimental Results: PARP cleavage increased in DU145 cells, and the effect was mo |
| Animal Protocol |
Animal/Disease Models: Nude mice with CWR22 xenografts [1]
Doses: 12 and 15 mg/kg Route of Administration: po (oral gavage); 12 and 15 mg/kg for 5 days, 2 days off; 13 days after tumor transplantation Results by day 37: No effect on tumor growth, but enhanced the effect of docetaxel on tumors. |
| References |
| Molecular Formula |
C19H16N2O3S2
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|---|---|
| Molecular Weight |
384.472
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| Exact Mass |
384.06
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| CAS # |
1233948-61-2
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| PubChem CID |
62705067
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
548.1±60.0 °C at 760 mmHg
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| Flash Point |
285.3±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.669
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| LogP |
5.01
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
616
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
STJKZARVVAISJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16N2O3S2/c1-13-3-4-14(15-9-17(11-20)25-12-15)10-19(13)21-26(22,23)18-7-5-16(24-2)6-8-18/h3-10,12,21H,1-2H3
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| Chemical Name |
N-(5-(5-cyanothiophen-3-yl)-2-methylphenyl)-4-methoxybenzenesulfonamide
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| Synonyms |
EL102; EL-102; EL 102.
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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 : ≥ 36 mg/mL (~93.64 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 | 2.6010 mL | 13.0049 mL | 26.0098 mL | |
| 5 mM | 0.5202 mL | 2.6010 mL | 5.2020 mL | |
| 10 mM | 0.2601 mL | 1.3005 mL | 2.6010 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.
 Impact of EL102 and docetaxel on prostate cancer cell line viabilityin vitro.(A) Chemical structure of EL102. (B) Dose response effects of EL102 on prostate cancer cell line viability over 72-h exposure. (C) Dose response effects of docetaxel on prostate cancer cell line viability over 72-h exposure. (D) Effect of EL102 on doxorubicin and docetaxel-resistant DLKPA lung cancer cell line viabilityvsDLKP parental lung cancer cell line. |
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 Impact of EL102 and docetaxel alone and in combination on CWR22 xenograft tumour volume.Br J Cancer. 2013 Oct 15; 109(8): 2131–2141. |
 Induction of cellular apoptosis by EL102 and docetaxel.Br J Cancer. 2013 Oct 15; 109(8): 2131–2141. |
 Impact of EL102 and docetaxel combination treatment on prostate cancer cell line viabilityin vitro.
EL102 inhibits Hif1αin normoxia and hypoxia.Br J Cancer. 2013 Oct 15; 109(8): 2131–2141. |
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 Cell cycle analysis of DU145 cell accumulation in G1, S, G2/M and subG1after EL102, docetaxel or combination treatment.
Representative cell cycle analysis of dose response effects of EL102-treated DU145.Br J Cancer. 2013 Oct 15; 109(8): 2131–2141. |
 Impact of EL102 and docetaxel alone and in combination on tubulin polymerisation activity.
Effect of EL102 on microtubule destabilisation.Br J Cancer. 2013 Oct 15; 109(8): 2131–2141. |
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