|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C26H21N3O2S |
||||||
| Molecular Weight | 439.53 | CAS No. | 948557-43-5 | ||||
| Solubility (25°C)* | In vitro | DMSO | 22 mg/mL (50.05 mM) | ||||
| Water | Insoluble | ||||||
| Ethanol | Insoluble | ||||||
| In vivo (Add solvents to the product individually and in order) |
|
||||||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
|||||||
Preparing Stock Solutions
Biological Activity
| Description | Tie2 kinase inhibitor 1 is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38. | ||
|---|---|---|---|
| Targets |
|
||
| In vitro | 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. [1] | ||
| In vivo | In 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. [1] |
Protocol (from reference)
| Animal Study:[1] |
|
|---|
Customer Product Validation
-
Data from [Neoplasia, 2012, 14, 131-40]
-
Data from [Neoplasia, 2012, 14, 131-40]
-
Data from [Data independently produced by , , Cancer Sci, 2018, 109(12):3805-3815]
Selleck's Tie2 kinase inhibitor 1 has been cited by 9 publications
| Neuroprotective effects of a novel peptide through the Rho-integrin-Tie2 and PI3K/Akt pathways in experimental autoimmune encephalomyelitis model [ Front Pharmacol, 2024, 15:1290128] | PubMed: 38384299 |
| Single-cell analysis reveals an Angpt4-initiated EPDC-EC-CM cellular coordination cascade during heart regeneration [ Protein Cell, 2023, 14(5):350-368] | PubMed: 37155312 |
| Tumor cell-derived exosomes deliver TIE2 protein to macrophages to promote angiogenesis in cervical cancer [ Cancer Lett, 2022, S0304-3835(22)00005-2] | PubMed: 35007697 |
| TIE2-high cervical cancer cells promote tumor angiogenesis by upregulating TIE2 and VEGFR2 in endothelial cells [ Transl Oncol, 2022, 26:101539] | PubMed: 36116242 |
| Angiopoietin-2 Promotes Inflammatory Activation in Monocytes of Systemic Sclerosis Patients [ Int J Mol Sci, 2020, 21(24)E9544] | PubMed: 33333969 |
| C16 Peptide Promotes Vascular Growth and Reduces Inflammation in a Neuromyelitis Optica Model [ Front Pharmacol, 2019, 10:1373] | PubMed: 31849648 |
| Phosphorylation of serine/arginine-rich splicing factor 1 at tyrosine 19 promotes cell proliferation in pediatric acute lymphoblastic leukemia [Xu L Cancer Sci, 2018, 109(12):3805-3815] | PubMed: 30320932 |
| Dual inhibition of EGFR and MET induces synthetic lethality in triple-negative breast cancer cells through downregulation of ribosomal protein S6 [ Int J Oncol, 2015, 47(1):122-32] | PubMed: 25955731 |
| Efficacy of Tie2 receptor antagonism in angiosarcoma. [Hasenstein JR, et al. Neoplasia, 2012, 14(2):131-40] | PubMed: 22431921 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.