Tie2 kinase inhibitor 1_product_DataBase

Bioactivity

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].

Target

IC50: 250 nM (Tie2)

Invitro

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:

Name

Tie2 kinase inhibitor 1

CAS

948557-43-5

Formula

C26H21N3O2S

Molar Mass

439.53

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

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

Reference

[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.

PeptideDB

Tie2 kinase inhibitor 1

CAS: 948557-43-5 F: C26H21N3O2S W: 439.53