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关于此项目
经验公式(希尔记法):
C17H12N4O2S
化学文摘社编号:
分子量:
336.37
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
[S](=O)(=O)(Nc2c3[nH]cc(c3c(cc2)C)C#N)c1cc(ccc1)C#N
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
ligand
E7820
assay
≥98% (HPLC)
form
powder
reaction suitability
reagent type: ligand
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
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.
inducer of selective proteasomal degradation of CAPERα
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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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