E 7820

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Cat.No. 6785 - E 7820 | C17H12N4O2S | CAS No. 289483-69-8
Description: α2 integrin inhibitor; anti-angiogenic
Chemical Name: 3-Cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

α2 integrin inhibitor. Inhibits angiogenesis in vitro (IC50 = 0.11 - 0.25 μM). Also inhibits growth of human colorectal cancer cell lines. Enhances efficacy of erlotinib in a non-small-cell lung cancer xenograft model. Also acts as a molecular glue to induce proteosomal degradation of mRNA splicing factor RBM39.

Technical Data

M. Wt 336.37
Formula C17H12N4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 289483-69-8
PubChem ID 196970
InChI Key LWGUASZLXHYWIV-UHFFFAOYSA-N
Smiles CC1=C2C(C#N)=CNC2=C(C=C1)NS(=O)(C3=CC(C#N)=CC=C3)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.64 100

Preparing Stock Solutions

The following data is based on the product molecular weight 336.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.97 mL 14.86 mL 29.73 mL
5 mM 0.59 mL 2.97 mL 5.95 mL
10 mM 0.3 mL 1.49 mL 2.97 mL
50 mM 0.06 mL 0.3 mL 0.59 mL

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References

References are publications that support the biological activity of the product.

Funahashi et al (2002) Sulfonamide derivative, E7820, is a unique angiogenesis inhibitor suppressing an expression of integrin α2 subunit on endothelium. Cancer Res. 62 6116

Ito et al (2014) 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. 105 1023 PMID: 24841832

Uehara et al (2017) Selective degradation of splicing factor CAPERα by anticancer sulfonamides. Nat.Chem.Biol. 13 675 PMID: 28437394


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Keywords: E 7820, E 7820 supplier, E7820, molecular, glue, targeted, protein, degradation, NSC719239, anti, angiogenesis, alpha2, integrin, inhibitors, inhibits, Integrins, Biochemicals, and, Molecular, Biology, 6785, Tocris Bioscience

Citations for E 7820

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Literature in this Area

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Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Enabling Research By Provision of Chemical Tools

Enabling Research By Provision of Chemical Tools Poster

The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.