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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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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, Glues, 6785, Tocris Bioscience
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