Tie2 kinase inhibitor 1

SKU: orb1300858

Description

Tie2 kinase inhibitor 1 is a potent and selective small molecule derived from SB-203580, exhibiting a 200-fold greater potency for Tie2 (IC50 = 0.25 µM) over p38 MAP kinase. This inhibitor is a valuable research tool for investigating Tie2 receptor signaling in angiogenesis, with applications in both cellular and preclinical in vivo models of cancer and vascular biology.

Research Area

Signal Transduction

Images & Validation

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Key Properties

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CAS Number	948557-43-5
MW	439.53
Purity	99.81%
Formula	C₂₆H₂₁N₃O₂S
SMILES	COc1ccc2cc(ccc2c1)-c1[nH]c(nc1-c1ccncc1)-c1ccc(cc1)S(C)=O
Target	Tie-2
Solubility	H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.28 mM);DMSO:4.4 mg/mL (10.01 mM)

Bioactivity

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Target IC50	Tie2:0.25 μM
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. Read more...
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. Read more...
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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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endothelial, internal, kinase, Tie2 kinase inhibitor 1, Tie-2 kinase inhibitor 1, Tie2, Tie-2, tunica

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Compound Identifiers

PubChem CID

23625762 ↗

Key Properties

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No computed properties available.

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