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Purity: ≥98%
E7820 (E-7820) is a novel and potent angiogenesis inhibitor and α2 integrin inhibitor with anticancer activity. It decreases integrin-α2 expression and is currently undergoing clinical trials. It is a small molecule and aromatic sulfonamide derivative with potential antiangiogenic and antitumor activities. E7820 inhibits angiogenesis by suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells. Inhibition of integrin alpha 2 leads to an inhibition of cell-cell interactions, endothelial cell-matrix interactions, vascular endothelial cell proliferation and angiogenesis. The combination of E7820 with erlotinib is an alternative strategy to overcome erlotinib resistance in NSCLC by enhancement of the anti-angiogenic activity of E7820.
| ln Vitro |
E7820 (ER68203-00) suppresses human umbilical vascular endothelial cell (HUVEC) ube production driven by both bFGF and VEGF in a dose-dependent manner, with IC50 values of 0.20 and 0.24 μg/ml, respectively[1]. E7820 prevents HUVEC from proliferating in serum-free medium (SFM) when it is stimulated by VEGF or bFGF. The respective IC50 values are 0.10 and 0.081 μg/ml. When compared to HUVEC, E7820's antiproliferative effect against WiDr and LoVo cells is incredibly weak. [1] The IC50 values were 15 and 29 μg/ml, respectively.
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| ln Vivo |
E7820 (ER68203-00) slows the proliferation of WiDr cells that have been injected with sc. (50-200 mg/kg; po; twice daily for 14 days)[1]. ?A powerful inhibitor of WiDr-induced angiogenesis, E7820 (200–400 mg/kg; po; once daily for 4 days) has been reported[1].
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| Animal Protocol |
Animal/Disease Models: Sixweeks old female nude mice (KSN mice, WiDr-induced angiogenesis model) [1]
Doses: 50, 100, 200 mg/kg Route of Administration: po; twice (two times) daily for 14 days from 2 days after inoculation of the tumor cells Experimental Results: The antitumor effect was dose-dependent at 50, 100, and 200 mg/kg, and the tumor growth rates were 52%, 46%, and 27%, respectively. |
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| References |
[1]. Funahashi Y, et al. Sulfonamide derivative, E7820, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. Cancer Res. 2002;62(21):6116-6123.
[2]. Ito K, et al. Enhanced anti-angiogenic effect of E7820 in combination with erlotinib in epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer xenograft models. Cancer Sci. 2014;105(8):1023-1031. |
| Molecular Formula |
C17H12N4O2S
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|---|---|
| Molecular Weight |
336.367781639099
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| CAS # |
289483-69-8
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| SMILES |
O=S(C1=CC=CC(C#N)=C1)(NC2=CC=C(C)C3=C2NC=C3C#N)=O
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| InChi Key |
LWGUASZLXHYWIV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12N4O2S/c1-11-5-6-15(17-16(11)13(9-19)10-20-17)21-24(22,23)14-4-2-3-12(7-14)8-18/h2-7,10,20-21H,1H3
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| Chemical Name |
N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide
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| Synonyms |
ER68203-00; E7820; ER 68203-00; E-7820; ER-68203-00; E 7820
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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 : ~100 mg/mL (~297.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9729 mL | 14.8646 mL | 29.7292 mL | |
| 5 mM | 0.5946 mL | 2.9729 mL | 5.9458 mL | |
| 10 mM | 0.2973 mL | 1.4865 mL | 2.9729 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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