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Tie2 kinase inhibitor 1

Catalog No. T6335 CAS 948557-43-5

Synonyms: Tie2 kinase inhibitor

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

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Tie2 kinase inhibitor 1 Chemical Structure

Tie2 kinase inhibitor 1, CAS 948557-43-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 62.00
2 mg	In stock	$ 88.00
5 mg	In stock	$ 189.00
10 mg	In stock	$ 313.00
25 mg	In stock	$ 537.00
50 mg	In stock	$ 775.00
100 mg	In stock	$ 1,080.00
500 mg	In stock	$ 2,170.00
1 mL * 10 mM (in DMSO)	In stock	$ 189.00

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Purity: 99.82%

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Description	Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor), an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.
Targets&IC50	Tie2:0.25 μM
In vitro	In HEL cells, Tie2 kinase inhibitor 1（IC50=232 nM） displays medium cellular activities. Tie2 kinase inhibitor 1 shows a medium inhibitory activity against Tie2 tyrosine kinase 1. Tie2 kinase inhibitor 1 is more specific for Tie2 than p38 (IC50=50 μM), and is a >10-fold specificity than VEGFR2, VEGFR3, and PDGFR1β.
In vivo	In a matrigel mouse model of angiogenesis, Tie2 kinase inhibitor 1 reduces angiogenesis. At doses of 25 and 50 mg/kg (i.p., b.i.d) for Tie2 kinase inhibitor 1, results on 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.
Kinase Assay	Enzymatic HDAC activity assays: 40 μL enzyme buffer (15 mM Tris HCl pH 8.1, 0.25 mM EDTA, 250 mM NaCl, 10% v:v glycerol) containing HDAC1, 3, 6 or 8 activity, 29 μL enzyme buffer and 1 μL resminostat at different concentrations are added to a 96-well microtitre plate and the reaction started by the addition of 30μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 6 μM for HDAC1, 10 μM for HDAC6 and 25 μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). After incubation for 3 hours (HDAC1, HDAC6, HDAC8) or 2 hours (HDAC3) at 30°C, the reaction is terminated by the addition of 25 μL stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/mL trypsin and 2 μM trichostatin A [TSA]). After incubation at room temperature for further 40 min, fluorescence is measured using a multilabel counter (extinction 355 nm, emission 460 nm) for quantification of AMC generated by tryptic cleavage of the deacetylated peptide. For the calculation of the IC50, the fluorescence in wells without test compound (1% DMSO, negative control) is set as 100% enzymatic activity and the fluorescence in wells with 2 μM TSA (positive control) is set at 0% enzymatic activity (background fluorescence substracted).
Animal Research	In MOPC-315 plasmacytoma xenograft model, Tie2 kinase inhibitor 1(≤50 mg), which is dissolved in 5% EtOH+5%cremophor+90% water, is injected intraperitoneally.

Synonyms	Tie2 kinase inhibitor
Molecular Weight	439.53
Formula	C26H21N3O2S
CAS No.	948557-43-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33 mg/mL (75.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Kinase Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library

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Related compounds with same targets

Pexmetinib TIE-2/VEGFR-2 kinase-IN-5 CE-245677 EOC317 Altiratinib BAY-826 Foretinib GSK-1070916

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Keywords

Tie2 kinase inhibitor 1 948557-43-5 Tyrosine Kinase/Adaptors Tie-2 internal Tie2 tumor Tie2 kinase inhibitor anti-cancer kinase inhibit Tie-2 kinase inhibitor 1 Inhibitor tunica endothelial inhibitor

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