ligand
E7820
质量水平
检测方案
≥98% (HPLC)
形式
powder
反应适用性
reagent type: ligand
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
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
InChI key
LWGUASZLXHYWIV-UHFFFAOYSA-N
生化/生理作用
E7820 (NSC 719239) is an orally available anticancer and antiangiogenic agent that inhibits VEGF-2 or FGF-2-induced tube formation of HUVEC cells through the suppression of integrin α2. E7820 promotes selective proteasomal degradation of the U2AF-related splicing factor CAPERα (coactivator of activating protein-1 and estrogen receptors) by ubiquitination and degradation via CRL4DCAF15.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Ron J Keizer et al.
The AAPS journal, 13(2), 230-239 (2011-03-10)
E7820 is an orally active inhibitor of α(2)-integrin mRNA expression, currently tested in phases I and II. We aimed to evaluate what levels of inhibition of integrin expression are needed to achieve tumor stasis in mice, and to compare this
Ken Ito et al.
Cancer science, 105(8), 1023-1031 (2014-05-21)
Most non-small-cell lung cancers (NSCLCs) harboring activating mutations in the epidermal growth factor receptor (EGFR) are initially responsive to EGFR tyrosine kinase inhibitors (EGFR-TKIs); however, they invariably develop resistance to these drugs. E7820 is an angiogenesis inhibitor that decreases integrin-α2
Taisuke Uehara et al.
Nature chemical biology, 13(6), 675-680 (2017-04-25)
Target-protein degradation is an emerging field in drug discovery and development. In particular, the substrate-receptor proteins of the cullin-ubiquitin ligase system play a key role in selective protein degradation, which is an essential component of the anti-myeloma activity of immunomodulatory
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