122520-86-9

122520-86-9 structure

Name: Tyrphostin 47
Chemical Name: 3-amino-2-[(3-hydroxy-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-3-sulfanylprop-2-enenitrile
CAS Number: 122520-86-9
Molecular Formula: C₁₀H₈N₂O₂S
Molecular Weight: 220.248
Catalog: Biochemical Amino acids and their derivatives Tyrosine derivatives
Create Date: 2018-06-14 11:53:09
Modify Date: 2024-01-05 13:31:08
Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells[1][2][3].

Name	3-amino-2-[(3-hydroxy-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-3-sulfanylprop-2-enenitrile
Synonyms	2-Propenethioamide, 2-cyano-3-(3,4-dihydroxyphenyl)-, (2E)- Tyrphostin 47 IN1038 (2E)-2-Cyano-3-(3,4-dihydroxyphenyl)-2-propenethioamide (2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enethioamide

Description	Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells[1][2][3].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
In Vitro	Tyrphostin AG213 (25 μM, 50 μM, 和 75 μM; 24 h, 48 h, 和 96 h) 增加人脐静脉内皮细胞 (HUVEC) 单层的伤口闭合时间[1]。 Tyrphostin AG213 (100 μM; 1 h) 干扰 HUVEC 焦点粘附和应力纤维形成[1]。 Tyrphostin AG213 (100 μM; 24 h) 抑制 HUVEC 中 pp125FAK 的粘附相关酪氨酸磷酸化[1]。 Tyrphostin AG213 (10 μM; 24 h) 抑制酪氨酸激酶活性，并且呈剂量和时间依赖关系地抑制 HT-29 细胞活力[2]。
References	[1]. Romer LH, et al. Tyrosine kinase activity, cytoskeletal organization, and motility in human vascular endothelial cells. Mol Biol Cell. 1994 Mar;5(3):349-61.