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Tie2 kinase inhibitor
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tie2 kinase inhibitor图片
CAS NO:948557-43-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)439.53
FormulaC26H21N3O2S
CAS No.948557-43-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 35 mg/mL (79.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)2% Cremophor EL, 2% N,N-dimethylacetamide: 30 mg/mL
Synonyms

Synonym: Tie2-inhibitor-5; Tie2 IN 5; Tie2IN5; Tie2 kinase inhibitor 5; Tie2-IN-5; Tie2 inhibitor 5; Compound 5;

Chemical Name: 4-[4-(6-Methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]pyridine

InChi Key: SINQIEAULQKUPD-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=S(C1=CC=C(C2=NC(C3=CC=C4C=C(OC)C=CC4=C3)=C(C5=CC=NC=C5)N2)C=C1)C

实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: Turned on an incubator shaker and adjusted temperature to 30 °C. Added 20 μL of 3× kinase buffer (final 20 mM Tris-HCl, pH 7, 100 mM NaCl, 12 mM MgCl2, 1 mM DTT) per well to the Flashplate. Added 20 μL of protein per well except for background. Added Tie2 Kinase Inhibitor, typically 1 ~ 2 μL in DMSO stocks. Added 20 μL of a mixture of gamma 33p-ATP and cold ATP (1:1 v/v) per well. Covered with transparent polyester film. Incubated at 30 °C for 2 hrs in shaker, washed five times. Read plate on TopCount or other counting instrument, and results were calculated as IC50 values using normal methods.


Cell Assay: In HEL cells, Tie2 Kinase Inhibitor moderately suppressed the activity of Tie2 tyrosine kinase, with an IC50 value of 232 NM.

In VivoIn 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.
Animal modelMOPC-315 plasmacytoma xenograft model.
Formulation & DosageDissolved in 5% EtOH+5%cremophor+90% water.; 50 mg/kg; i.p. injection
References

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60