Tie2 kinase inhibitor 1

製品コードS1577 バッチS157702

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₂₁N₃O₂S

分子量

439.53

CAS No.

948557-43-5

Solubility (25°C)*

体外

DMSO

22 mg/mL (50.05 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

2% Cremophor EL 1 2% N 2 N-dimethylacetamide

30.0mg/ml

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ	Tie2 kinase activity assay
キナーゼアッセイ	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.

参考

[1] Semones M, et al. Bioorg Med Chem Lett, 2007, 17(17), 4756-4760.

カスタマーフィードバック

: 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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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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