Tie2 kinase inhibitor

Product Name: 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;4-(6-Methoxy-2-naphthyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole;4-(4-(6-Methoxynaphthalen-2-yl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine;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;Pyridine, 4-[4-(6-methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]-
CBNumber: CB02510437
Molecular Formula: C26H21N3O2S
Formula Weight: 439.53
MOL File: 948557-43-5.mol

More

Less

Tie2 kinase inhibitor Property

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

More

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

More

Less

N-Bromosuccinimide Price

Cayman Chemical

Product number: 17858
Product name: Tie2 Kinase Inhibitor
Purity: ≥95%
Packaging: 500μg
Price: $40
Updated: 2024/03/01

Cayman Chemical

Product number: 17858
Product name: Tie2 Kinase Inhibitor
Purity: ≥95%
Packaging: 1mg
Price: $64
Updated: 2024/03/01

Cayman Chemical

Product number: 17858
Product name: Tie2 Kinase Inhibitor
Purity: ≥95%
Packaging: 5mg
Price: $195
Updated: 2024/03/01

Cayman Chemical

Product number: 17858
Product name: Tie2 Kinase Inhibitor
Purity: ≥95%
Packaging: 10mg
Price: $351
Updated: 2024/03/01

TRC

Product number: M264745
Product name: 4-(6-Methoxy-2-naphthyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole
Packaging: 10mg
Price: $295
Updated: 2021/12/16

More

Less

Tie2 kinase inhibitor Chemical Properties,Usage,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

More

Less

Tie2 kinase inhibitor Suppliers

Canada 1 China 80 India 2 United States 9 Global 92

AdooQ BioScience, LLC

Tel: +1 (866) 930-6790
Fax: +1 (866) 333-9607
Email: info@adooq.com
Country: United States
ProdList: 2782
Advantage: 58

Target molecule Corp.

Tel: 857-239-0968
Fax: 857-239-8801
Email: service1@targetmol.com
Country: United States
ProdList: 2559
Advantage: 60

InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6391
Advantage: 58

Aladdin Scientific

Tel: +1-+1(833)-552-7181
Email: sales@aladdinsci.com
Country: United States
ProdList: 57505
Advantage: 58

TargetMol Chemicals Inc.

Tel
Email: support@targetmol.com
Country: United States
ProdList: 38632
Advantage: 58

ApexBio Technology

Tel: --
Fax: --
Email: sales@apexbt.com
Country: United States
ProdList: 6251
Advantage: 58

Cayman Chemical Company

Tel: --
Fax: --
Email: cayman@caymanchem.com
Country: United States
ProdList: 6213
Advantage: 81

Creative Enzymes

Tel: --
Fax: --
Email: info@creative-enzymes.com
Country: United States
ProdList: 6057
Advantage: 58

MedChemExpress

Tel: --
Fax: --
Email: sales@medchemexpress.com
Country: United States
ProdList: 6398
Advantage: 58

948557-43-5, Tie2 kinase inhibitorRelated Search:

EC 2.7.1.40 STREPTOKINASE 1L-6-HYDROXYMETHYL-CHIRO-INOSITOL 2-(R)-2-O-METHYL-3-O-OCTADECYLCARBONATE JAK INHIBITOR I NADH Inhibitor RIBONUCLEASE INHIBITOR Everolimus Y27632 (hydrochloride) Bosutinib BAY 87-2243 S3I-201 GW441756

Tie2 kinase inhibitor

4-[4-(6-Methoxy-2-naphthalenyl)-2-[4-(Methylsulfinyl)phenyl]-1H-iMidazol-5-yl]pyridine

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

Tie2 kinase-IN-1

Tie2 kinase inhibitor 1

4-(4-(6-Methoxynaphthalen-2-yl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine

Pyridine, 4-[4-(6-methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]-

Tie2 kinase inhibitor USP/EP/BP

948557-43-5

Aromatics

Heterocycles

Inhibitors

Intermediates & Fine Chemicals

Pharmaceuticals

Sulfur & Selenium Compounds