ATN-161

製品コードS8454 バッチS845401

印刷

化学情報

Chemical Structure Synonyms Ac-PHSCN-NH2 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H35N9O8S
分子量 597.64 CAS No. 262438-43-7
Solubility (25°C)* 体外 Water 13 mg/mL (21.75 mM)
 
 
* <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 ATN-161 is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
in vitro ATN-161 interacts with the N-terminus of the β1-domain of integrin α5β1, which may lock this integrin in an inactive conformation[2]. ATN-161 treatment up to 100 μmol/L shows no significant effect on tumor cell proliferation compared with the vehicle-treated control group of cells. However, ATN-161 significantly inhibits MAPK phosphorylation with maximal effects observed at 20 μmol/L of ATN-161 after 30 minutes of treatment[1].
in vivo ATN-161 (Ac-PHSCN-NH2), a 5-mer capped peptide derived from the synergy region of fibronectin that binds to α5β1 and αvβ3 in vitro, blocks breast cancer growth and metastasis. Treatment with ATN-161 causes a significant dose-dependent decrease in tumor volume and either completely blocked or caused a marked decrease in the incidence and number of skeletal as well as soft tissue metastases. Treatment with ATN-161 results in a significant decrease in the expression of phosphorylated mitogen-activated protein kinase, microvessel density, and cell proliferation in tumors grown in vivo[1]. ATN-161 is a peptide with a fairly short plasma half-life. compared with the plasma pharmacokinetics of ATN-161, It is cleared from the tumor with much slower kinetics supporting the hypothesis that this peptide exerts its effects through a durable interaction with its target(s)in the tumor[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MDA-MB-231 cells
濃度 1-100 μmol/L
反応時間 15-60 minutes
実験の流れ

MDA-MB-231 (1 × 106) cells are plated in 100 mm Petri dishes for 24 hours, then serum-starved overnight before treatment with vehicle or ATN-161 (1-100 μmol/L) for different time periods (15-60 minutes). Western blot analyses are carried out using antibodies against focal adhesion kinase, phosphorylated FAK, mitogen-activated protein kinase (MAPK), phosphorylated MAPK, and β-tubulin as previously described. Western blots are detected using enhanced chemiluminescence detection reagents.
動物実験 動物モデル BALB/c nu/nu mice
投薬量 0.05-1 mg/kg/d
投与方法 i.v.

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：

Ion elemental-optimized layered double hydroxide nanoparticles promote chondrogenic differentiation and intervertebral disc regeneration of mesenchymal stem cells through focal adhesion signaling pathway [ Bioact Mater, 2023, 22:75-90] PubMed: 36203960
Tumor-derived insulin-like growth factor-binding protein-1 contributes to resistance of hepatocellular carcinoma to tyrosine kinase inhibitors [ Cancer Commun (Lond), 2023, 10.1002/cac2.12411] PubMed: 36825684
Stromal-induced epithelial-mesenchymal transition induces targetable drug resistance in acute lymphoblastic leukemia [ Cell Rep, 2023, 42(7):112804] PubMed: 37453060
Targeting NADPH Oxidase and Integrin α5β1 to Inhibit Neutrophil Extracellular Traps-Mediated Metastasis in Colorectal Cancer [ Int J Mol Sci, 2023, 10.3390/ijms242116001] PubMed: 37958984
SHARPIN Enhances Ferroptosis in Synovial Sarcoma Cells via NF-κB- and PRMT5-Mediated PGC1α Reduction [ Cancers (Basel), 2023, 15(13)3484] PubMed: 37444594
The natural compound atraric acid suppresses androgen-regulated neo-angiogenesis of castration-resistant prostate cancer through angiopoietin 2 [ Oncogene, 2022, 10.1038/s41388-022-02333-7] PubMed: 35513564
EXOC4 Promotes Diffuse-Type Gastric Cancer Metastasis via Activating FAK Signal [ Mol Cancer Res, 2022, 20(7):1021-1034] PubMed: 35471457
EXOC4 Promotes Diffuse-Type Gastric Cancer Metastasis via Activating FAK Signal [ Mol Cancer Res, 2022, 20(7):1021-1034] PubMed: 35471457
ITGA5 and ITGB1 contribute to Sorafenib resistance by promoting vasculogenic mimicry formation in hepatocellular carcinoma [ Cancer Med, 2022, 10.1002/cam4.5110] PubMed: 35946175
Phosphorylation inhibition of protein-tyrosine phosphatase 1B tyrosine-152 induces bone regeneration coupled with angiogenesis for bone tissue engineering [ Bioact Mater, 2021, 6(7):2039-2057] PubMed: 33511306

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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