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ligand
E7820
品質等級
化驗
≥98% (HPLC)
形狀
powder
反應適用性
reagent type: ligand
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
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 密鑰
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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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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