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Tie2 kinase inhibitor

Names

[ CAS No. ]:
948557-43-5

[ Name ]:
Tie2 kinase inhibitor

[Synonym ]:
S1577_Selleck
X7496
4-{4-(6-Methoxy-2-naphthyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl}pyridine
Tie2 kinase inhibitor-Supplied by Selleck Chemicals
4-{4-(6-methoxynaphthalen-2-yl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl}pyridine
Pyridine, 4-[4-(6-methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]-
Tie2 kinase inhibitor

Biological Activity

[Description]:

Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM[1]. Tie2 kinase inhibitor 1 has anti-cancer activity[2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[Target]

IC50: 250 nM (Tie2)[1]


[In Vitro]

Tie2 kinase inhibitor 1 (compound 5) has an IC50 of 50 μM for p38 and has moderate to excellent cellular activities (cell IC50=232 nM)[1]. Tie2 kinase inhibitor 1 inhibits tunica internal endothelial cell kinase 2 (Tie2)[2].

[In Vivo]

Tie2 kinase inhibitor 1 (intraperitoneally; 50 mg/kg; twice a week for 6 weeks) results in statistically significant reductions in tumor volume by day 15. Tie2 kinase inhibitor 1 results in a 61% reduction in tumor volume by day 20, and reduces tumor volume by 45% by 6 weeks[1]. Animal Model: Athymic nude mice (6- to 8-week-old females)[1] Dosage: 50 mg/kg Administration: Intraperitoneally; twice a week for 6 weeks Result: Resulted in statistically significant reductions in tumor volume.

[References]

[1]. Semones M, et al. Pyridinylimidazole inhibitors of Tie2 kinase. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60. Epub 2007 Jun 27.

[2]. Hasenstein JR, et al. Efficacy of Tie2 receptor antagonism in angiosarcoma. Neoplasia. 2012 Feb;14(2):131-40.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
699.8±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H21N3O2S

[ Molecular Weight ]:
439.529

[ Flash Point ]:
377.0±31.5 °C

[ Exact Mass ]:
439.135437

[ PSA ]:
87.08000

[ LogP ]:
5.31

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.746

[ Storage condition ]:
-20℃

Safety Information

[ Hazard Codes ]:
N

Related Compounds