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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H21N3O2S |
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分子量 | 439.53 | CAS No. | 948557-43-5 | |
Solubility (25°C)* | 体外 | 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. |
製品説明 | 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. |
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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] |
キナーゼアッセイ | Tie2 kinase activity assay | |
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Turn on an incubator shaker and adjust temperature to 30 °C. Add 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. Add 20 μL of protein per well except for background. Add Tie2 kinase inhibitor, typically 1-2 μL in DMSO stocks. Add 20 μL of a mixture of gamma 33p-ATP and cold ATP(1:1 v/v ) per well. Cover with transparent polyester film. Incubate at 30 °C for 2 hours in shaker, wash five times. Read plate on TopCount or other counting instrument, results are calculated as IC50 using normal methods. | ||
動物実験 | 動物モデル | MOPC-315 plasmacytoma xenograft model. |
投薬量 | ≤50 mg | |
投与方法 | Administered via i.p. |
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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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