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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 |
[1]. A P Toner et al. The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivoactivity against prostate cancer and circumvents MDR1 resistance. Br J Cancer, 2013 Oct 15, 109(8): 2131-2141.
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| Molecular Formula |
C19H16N2O3S2
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| Molecular Weight |
384.472
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| CAS # |
1233948-61-2
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| SMILES |
C1=CC(C2C=C(C#N)SC=2)=CC(NS(=O)(=O)C2=CC=C(OC)C=C2)=C1C
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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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| 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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| 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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