Tie2 kinase inhibitor
- CAS No.
- 948557-43-5
- Chemical Name:
- Tie2 kinase inhibitor
- Synonyms
- Tie2 kinase-IN-1;Tie2 kinase inhibitor;Tie2 kinase inhibitor 1;Tie2 kinase inhibitor USP/EP/BP;Tie2 kinase inhibitor（948557-43-5）;Tie2 kinase inhibitor 1, 10 mM in DMSO;4-(6-Methoxy-2-naphthyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole;4-(5-(6-methoxynaphthalen-2-yl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-4-yl)pyridine;4-[4-(6-Methoxy-2-naphthalenyl)-2-[4-(Methylsulfinyl)phenyl]-1H-iMidazol-5-yl]pyridine;4-(4-(6-Methoxynaphthalen-2-yl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine
- CBNumber:
- CB02510437
- Molecular Formula:
- C26H21N3O2S
- Molecular Weight:
- 439.53
- MDL Number:
- MFCD14585804
- MOL File:
- 948557-43-5.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Boiling point | 699.8±55.0 °C(Predicted) |
|---|---|
| Density | 1.39±0.1 g/cm3(Predicted) |
| storage temp. | 2-8°C(protect from light) |
| solubility | ≥22 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| form | Powder |
| pka | 9.53±0.10(Predicted) |
| color | Light yellow to yellow |
| InChI | 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) |
| InChIKey | SINQIEAULQKUPD-UHFFFAOYSA-N |
| SMILES | C1=NC=CC(C2NC(C3=CC=C(S(C)=O)C=C3)=NC=2C2=CC=C3C(=C2)C=CC(OC)=C3)=C1 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501 | |||||||||
| NFPA 704 |
|
Tie2 kinase inhibitor price More Price(56)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 17858 | Tie2 Kinase Inhibitor ≥95% | 948557-43-5 | 500μg | $44 | 2026-04-30 | Buy |
| Cayman Chemical | 17858 | Tie2 Kinase Inhibitor ≥95% | 948557-43-5 | 1mg | $71 | 2026-04-30 | Buy |
| Cayman Chemical | 17858 | Tie2 Kinase Inhibitor ≥95% | 948557-43-5 | 5mg | $215 | 2026-04-30 | Buy |
| Cayman Chemical | 17858 | Tie2 Kinase Inhibitor ≥95% | 948557-43-5 | 10mg | $387 | 2026-04-30 | Buy |
| Usbiological | 016314 | 4-(6-Methoxy-2-naphthyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole | 948557-43-5 | 10mg | $446 | 2026-06-03 | Buy |
Tie2 kinase inhibitor Chemical Properties, Uses, Production
Uses
Tie2 kinase inhibitor.
Uses
Tunica interna endothelial cell kinase 2 (Tie2, also known as angiopoietin-1 receptor or tek) is an endothelium-specific receptor tyrosine kinase important for the development of embryonic vasculature and for angiogenesis and vascular maintenance in adult tissues. Tie2 kinase inhibitor reversibly and selectively blocks Tie2 kinase activity with an IC50 value of 250 nM. It is 200-fold more potent for inhibition of Tie2 compared to p38. Tie2 kinase inhibitor has been shown to reduce angiogenesis in a Matrigel neovascularization assay and to delay tumor growth in MOPC-315 plasmacytoma and SVR angiosarcoma xenograft models.[Cayman Chemical]
Definition
ChEBI: 4-[4-(6-methoxy-2-naphthalenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine is a member of imidazoles.
Biological Activity
genetic studies have identified the crucial roles of tie receptors (tie1 & tie2) in the development and function of endothelial tissues, including promoting the survival, maturation and functional integrity of the vasculature. tie2 kinase inhibitor is suggested to block vascular construction via suppressing tie2, and in this way it is expected to disrupt tumor growth and angiogenesis. [1]
in vitro
tie2 kinase inhibitor exhibited significant inhibitory effect on tie2 auto-phosphorylation and disrupted its downstream signal transduction in a dose dependent manner in human aortic endothelial cells. in addition, tie2 kinase inhibitor exhibits moderately suppressed the activity of tie2 tyrosine kinase in hel cells with ic50 of 232 nm. [2, 3]
in vivo
matrigel mouse model of angiogenesis was adopted for in vivo study. tie2 kinase inhibitor at doses of 25 and 50 mg/kg (i.p., b.i.d) reduced 41% and 70% of angiogenesis, respectively. in a mopc-315 plasmacytoma xenograft model, tie2 kinase inhibitor modestly suppressed tumor growth in nude mice in a dose-dependent manner. [4]
IC 50
a reversible and selective inhibitor of tie2 with ic50 of 0.25 m, whose selectivity is 200-fold higher than that of p38.
References
[1] lagreca s, arcari j, baker d, borzillo g, chen j, clark t, cohen b, hungerford w, kakar s, kanter a, knauth k, lu y, martinez-alsina l, marx m, patel n, soderstrom c, tkalcevic g, thompson c, troutman m, vincent p, wessel m. identification of selective, orally active tie2 kinase inhibitors and discovery of ce-245,677 and pf-371,989. cancer res. 2007 may; 67: 3259.
[2] liu l , lina t, coleb a, wenc r, zhao l, bresciab mr, jacoba b, hussainb z, appella k, hendersonb i, webba m. dentification and characterization of small-molecule inhibitors of tie2 kinase. febs lett. 2008 mar; 582(5): 785-91.
[3] semones m, feng y, johnson n, adams jl, winkler j, hansbury m. pyridinylimidazole inhibitors of tie2 kinase. bioorg med chem lett. 2007 sep; 17(17): 4756-60.
[4]hasenstein jr, kasmerchak k, buehler d, hafez gr, claery k, moody js, kozak kr. efficacy of tie2 receptor antagonism in angiosarcoma. neoplasia 2012 feb;14(2):131-40.
[5] garcia-manero g, khoury hj, jabbour e, lancet j, winski sl, cable l, rush s, maloney l, hogeland g, ptaszynski m, calvo mc, bohannan z, kantarjian h, komrokji r. a phase i study of oral arry-614, a p38 mapk/tie2 dual inhibitor, in patients with low or intermediate-1 risk myelodysplastic syndromes. clin cancer res. 2015 mar 1;21(5):985-94.
Tie2 kinase inhibitor Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Angel Pharmatech, Ltd. | 17317130613 | 3358272972@qq.com | China | 3307 | 58 |
| J & K SCIENTIFIC LTD. | 18210857532 18210857532 | jkinfo@jkchemical.com | China | 96815 | 76 |
| Chemsky (shanghai) International Co.,Ltd | 021-50135380 | shchemsky@sina.com | China | 15350 | 60 |
| Jinan Trio PharmaTech Co., Ltd. | 0531-88811783 | sales@trio-pharmatech.com | China | 1856 | 62 |
| NCE Biomedical Co.,Ltd. | 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 | China | 1490 | 55 | |
| Shanghai Aladdin Bio-Chem Technology Co.,LTD | 400-6206333 13167063860 | anhua.mao@aladdin-e.com | China | 29977 | 65 |
| The future of Shanghai Industrial Co., Ltd. | 021-61552785 | sales@shshiji.com | China | 9531 | 55 |
| AdooQ BioScience, LLC | +1 (866) 930-6790 | info@adooq.com | United States | 2774 | 58 |
| Bide Pharmatech Ltd. | 400-164-7117 18317119277 | product02@bidepharm.com | China | 40000 | 60 |
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7717 | 56 |
