Tie2 kinase inhibitor

Catalog No.S1577

Tie2 kinase inhibitor Chemical Structure

Molecular Weight(MW): 439.53

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

Size Price Stock Quantity  
In DMSO USD 490 In stock
USD 380 In stock
USD 980 In stock
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Cited by 2 Publications

3 Customer Reviews

  • Inhibition of SVR (solid line) and MS1-VEGF (dashed line) cell survival by sunitinib (A) and Tie2 kinase inhibitor (B) and dose effect analysis of combined sunitinib and Tie2 kinase inhibitor (C). Cell survival was determined as described in Materials and Methods. Combination indices <1, =1, and >1 denote synergy, additivity, and antagonism, respectively. Values represent mean ?SE (n = 4).

    Neoplasia 2012 14, 131-40. Tie2 kinase inhibitor purchased from Selleck.

    In vivo SVR (A) and MS1-VEGF (B) tumor growth inhibition with sunitinib, Tie2 kinase inhibitor, and combination. Tumor-bearing mice were treated as described in Materials and Methods (SVRn =5,MS1-VEGF n =4).*P < 0.05, control versus each treatment group.

    Neoplasia 2012 14, 131-40. Tie2 kinase inhibitor purchased from Selleck.

  • Cytotoxicity of Tie2 kinase inhibitor. A, Cytotoxicity assays were undertaken with varying concentrations (0‐200 μmol/L) of Tie2 kinase inhibitor. Relative cell viabilities were plotted in GraphPad Prism 6 using a variable slope logistic curve. B, Viabilities of Nalm‐6 stable cells overexpressing SRSF1‐WT were compared between cells treated with Tie2 inhibitor (200 μmol/L) and the negative control (NC). C, Colony formation assays were undertaken with the treated Tie2 inhibitor (10 μmol/L), cells treated with DMSO were used as NC. D, Number of clones was counted. Inhibition rates of colony formation between Tie2 inhibitor and NC groups for each stable cell were compared. Bar represents SEM. Each experiment performed in triplicate. *P < .05, **P < .01

    Cancer Sci, 2018, 109(12):3805-3815. Tie2 kinase inhibitor purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Tie2 kinase inhibitor 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

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 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]

Protocol

Animal Research:[1]
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  • Animal Models: MOPC-315 plasmacytoma xenograft model.
  • Formulation: Tie2 kinase inhibitor is dissolved in 5% EtOH+5%cremophor+90% water.
  • Dosages: ≤50 mg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL (79.63 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% Cremophor EL, 2% N,N-dimethylacetamide
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 439.53
Formula

C26H21N3O2S

CAS No. 948557-43-5
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Tie-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID