- E7820
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- $30.00 / 1mg
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2025-07-14
- CAS:289483-69-8
- Min. Order:
- Purity: 99.11%
- Supply Ability: 10g
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| Product Name: | E-7820 | | Synonyms: | E-7820;ER 68203-00;3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide;N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide;E 7820; E-7820;CS-2701;ER68203-00;E7820;E-7820;E 7820;289483-69-8;Benzenesulfonamide, 3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)- | | CAS: | 289483-69-8 | | MF: | C17H12N4O2S | | MW: | 336.37 | | EINECS: | | | Product Categories: | | | Mol File: | 289483-69-8.mol |  |
| | E-7820 Chemical Properties |
| Boiling point | 626.2±65.0 °C(Predicted) | | density | 1.48±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:67.0(Max Conc. mg/mL);199.19(Max Conc. mM) | | form | A crystalline solid | | pka | 8.17±0.30(Predicted) | | color | Light yellow to light brown | | InChI | 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 | | InChIKey | LWGUASZLXHYWIV-UHFFFAOYSA-N | | SMILES | C1(S(NC2C3=C(C(C)=CC=2)C(C#N)=CN3)(=O)=O)=CC=CC(C#N)=C1 |
| | E-7820 Usage And Synthesis |
| Description | E7820 is a sulfonamide derivative and an angiogenesis inhibitor that inhibits bFGF- and VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation (IC50s = 0.1 and 0.081 μg/ml, respectively). It inhibits bFGF- and VEGF-stimulated tube formation of HUVECs in a concentration-dependent manner (IC50s = 0.2 and 0.24 μg/ml, respectively). E7820 selectively decreases the surface expression and mRNA levels of integrin α2 over CD31 and VE-cadherin in HUVECs. In vivo, E7820 (200 and 400 mg/kg) reduces tumor growth and inhibits angiogenesis in a WiDr colorectal cancer mouse xenograft model. It also reduces tumor weight in a panel of seven human colon, breast, pancreas, and kidney cancer mouse xenograft models, completely inhibits tumor growth in KP-1 pancreatic and LoVo colon cancer mouse xenograft models, and inhibits tumor growth in KP-1 and COLO 320DM mouse orthotopic transplantation models. | | Uses | E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity[1][2]. | | reaction suitability | reagent type: ligand | | in vivo | E7820 (ER68203-00) (50-200 mg/kg; p.o. ; twice daily for 14 days) delays the growth of WiDr cells inoculated s.c.[1].
E7820 (200-400 mg/kg; p.o.;once daily for 4 days) potently inhibits WiDr-induced angiogenesis[1]. | Animal Model: | Six-week-old female nude mice (KSN mice, WiDr-induced angiogenesis model) [1] | | Dosage: | 50, 100, 200 mg/kg | | Administration: | p.o. ; twice daily for 14 days from 2 days after inoculation of the tumor cells | | Result: | 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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| | storage | Store at -20°C | | 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. PMID:12414636
[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. DOI:10.1111/cas.12450 |
| | E-7820 Preparation Products And Raw materials |
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