AG-213 (Synonyms:酪氨酸磷酸化抑制剂A47;酪氨酸磷酸化抑制剂;酪氨酸磷酸化抑制剂AG 213)
目录号 : KCM10738 CAS No. : 122520-86-9 纯度 : ≥97%
Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. AG-213 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC value of 2.4 µM in the human epidermoid carcinoma cell line A431.
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生物活性

AG-213 is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). AG-213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). TAG-213 can induce nonapoptotic cell programmed death in tumor cells,

体外研究

AG-213 (25 μM, 50 μM, and 75 μM; 24 h, 48 h, and 96 h) increases wound closure time in human umbilical vein endothelial cell (HUVEC) monolayer.

AG-213 (100 μM; 1 h) interferes with HUVEC focal adhesion and stress fiber formation.

AG-213 (100 μM; 24 h) inhibits adherence-related tyrosine phosphorylation of pp125FAK in HUVEC.

AG-213 (10 μM; 24 h) inhibits tyrosine kinase activity, and (4.55-455 mM; 24-72 h) inhibits HT-29 cell viability doseand time-dependently.

分子式
C10H8N2O2S
分子量
220.2
CAS号
122520-86-9
中文名称
酪氨酸磷酸化抑制剂A47
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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