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Submit ReviewE 7820 is a 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.
E 7820 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 336.37 |
公式 | C17H12N4O2S |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 33.64 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for E 7820, please let us know.
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