Tie2 kinase inhibitor

Tie2-IN-5 is a reversible and selective ATP-binding site-targeting Tie2 kinase inhibitor.

Product information

CAS Number: 948557-43-5

Molecular Weight: 439.53

Formula: C26H21N3O2S

Synonym:

Tie2-IN-5

Tie2 IN 5

Tie2IN5

Tie2 inhibitor 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

Smiles: COC1=CC2=CC=C(C=C2C=C1)C1N=C(NC=1C1C=CN=CC=1)C1C=CC(=CC=1)S(C)=O

InChiKey: SINQIEAULQKUPD-UHFFFAOYSA-N

InChi: InChI=1S/C26H21N3O2S/c1-31-22-8-5-19-15-21(4-3-20(19)16-22)25-24(17-11-13-27-14-12-17)28-26(29-25)18-6-9-23(10-7-18)32(2)30/h3-16H,1-2H3,(H,28,29)

Technical Data

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: ≥12 months 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

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].

References:

1. Semones M, et al. Bioorg Med Chem Lett, 2007, 17(17), 4756-4760.
2. 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.