Tie2 kinase inhibitor 1

Catalog No.S1577 Batch:S157701

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Technical Data

Formula

C26H21N3O2S

Molecular Weight 439.53 CAS No. 948557-43-5
Solubility (25°C)* In vitro DMSO 35 mg/mL (79.63 mM)
Water Insoluble
Ethanol Insoluble
* <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.)

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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
Tie-2 [1]
0.25 μM
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]
  • Animal Models

    MOPC-315 plasmacytoma xenograft model.

  • Dosages

    ≤50 mg

  • Administration

    Administered via i.p.

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

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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.