Tie2-IN-5 is a reversible and selective ATP-binding site-targeting Tie2 kinase inhibitor.
CAS Number: 948557-43-5
Molecular Weight: 439.53
Tie2 IN 5
Tie2 inhibitor 5
Tie2 kinase inhibitor 5
Chemical Name: 4-[4-(6-Methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]pyridine
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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). Tie2 kinase inhibitor 1 inhibits tunica internal endothelial cell kinase 2 (Tie2).
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.
- Semones M, et al. Bioorg Med Chem Lett, 2007, 17(17), 4756-4760.
- Hasenstein JR, et al. Efficacy of Tie2 receptor antagonism in angiosarcoma. Neoplasia. 2012 Feb;14(2):131-40.
Products are for research use only. Not for human use.
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