Home Protein Tyrosine Kinase Tie-2 inhibitor Tie2 kinase inhibitor 1 For research use only.

Tie2 kinase inhibitor 1

Tie2 kinase inhibitor 1 is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.

Tie2 kinase inhibitor 1 Chemical Structure

Tie2 kinase inhibitor 1 Chemical Structure

CAS: 948557-43-5

Selleck's Tie2 kinase inhibitor 1 has been cited by 8 Publications

3 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Signaling Pathway

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Biological Activity

Description Tie2 kinase inhibitor 1 is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.
Targets
Tie-2 [1]
0.25 μM
In vitro
In vitro Tie2 kinase inhibitor exhibits a moderate inhibitory activity against Tie2 tyrosine kinase. Tie2 kinase inhibitor also shows moderate cellular activities with IC50 of 232 nM in HEL cells. Furthermore, Tie2 kinase inhibitor has a remarkable selectivity for Tie2 over p38 (IC50=50 μM) and a >10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1β. [1]
In Vivo
In vivo In a Matrigel mouse model of angiogenesis, Tie2 kinase inhibitor, at doses of 25 and 50 mg/kg (i.p., b.i.d), leads to a reduction of 41% and 70% of angiogenesis, respectively. In a MOPC-315 plasmacytoma xenograft model, Tie2 kinase inhibitor treatment results in a modest dose dependent delay in tumor growth. [1]
Animal Research Animal Models MOPC-315 plasmacytoma xenograft model.
Dosages ≤50 mg
Administration Administered via i.p.

Chemical Information & Solubility

Molecular Weight 439.53 Formula

C26H21N3O2S
CAS No. 948557-43-5 SDF Download Tie2 kinase inhibitor 1 SDF
Smiles COC1=CC2=C(C=C1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)S(=O)C)C5=CC=NC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 35 mg/mL ( (79.63 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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