Tyrphostin 47

Names

[ Name ]:
Tyrphostin 47

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
474.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₀H₈N₂O₂S

[ Molecular Weight ]:
220.248

[ Flash Point ]:
240.8±31.5 °C

[ Exact Mass ]:
220.030655

[ PSA ]:
122.36000

[ LogP ]:
0.93

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.780

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: 50 mg/mL, clear, orange

Safety Information

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
26-36

[ WGK Germany ]:
3

Related Compounds

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