Y15

製品コードS5321 バッチS532102

印刷

化学情報

Chemical Structure Synonyms 1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C6H10N4.4HCl
分子量 284.01 CAS No. 4506-66-5
Solubility (25°C)* 体外 Water 28 mg/mL (98.58 mM)
DMSO 19 mg/mL (66.89 mM)
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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
in vitro Y15 treatment in vitro results in decreased cell viability, increased detachment, and increased apoptosis in colon cancer cells, breast cancer cells, and melanoma. In TPC1, BCPAP, K1 and TT cell lines, Y15 inhibits pY397 and total FAK expression in a dose-dependent manner. It causes effective dose-dependent detachment in all thyroid cancer cell lines. Y15 causes dose-dependent decrease of colony formation in all papillary thyroid cancer cell lines and increases necrosis in papillary and medullary thyroid cancer cell lines[1]. Y15 does not target homologous Pyk-2, c-Src, c-RAF, EGFR, IGFR, PDGFR, PI3K, VEGFR-3, and c-Met[3].
in vivo Y15 blocks breast, pancreatic and neuroblastoma tumor growth in vivo[2]. The pharmacokinetics study in mice demonstrates that, following intraperitoneal administration at 30 mg/kg dose, Y15 is very rapidly absorbed in mice, reaching maximum plasma concentration in 4.8 min. Y15 rapidly metabolizes in mouse and human liver microsomes with half-life t1/2 of 6.9 and 11.6 min, respectively. The maximal tolerated dose of single-dose administration of Y15 by oral administration is 200 mg/kg, and the multiple maximum tolerated dose of Y15 is 100 mg/kg by PO during 7 day study. Y15 does not cause any mortality or statistically significant differences in the body weight at 30 mg/kg by IP during 28-day study, and at 100 mg/kg by PO during the 7-day study. There are no clinical chemical, hematological, or histopathological changes in different mice organs at 30 mg/kg by IP during 28 days and at 100 mg/kg dose by PO during 7 days[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 The thyroid cancer cell lines: TPC1, TT and BCPAP
濃度 0-50 μM
反応時間 24 h
実験の流れ Cells are seeded onto 96-well plates (10,000 cells per well in 100 μL of medium plus 10% FBS and 1% penicillin/streptomycin). Twenty-four hours following inhibitor treatment, 20 μL of Cell Titer 96 Aqueous One Solution Cell Proliferation Assay is added to each well. After two hours of incubation with reagent and the plate is read at 490 nm.
動物実験 動物モデル The CD-1 albino mice; 7 weeks old (males) and 9 weeks old (females)
投薬量 30 mg/kg or 100 mg/kg
投与方法 intraperitoneal (IP) or oral (PO) delivery

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：

FNBP1 Facilitates Cervical Cancer Cell Survival by the Constitutive Activation of FAK/PI3K/AKT/mTOR Signaling [ Cells, 2023, 12(15)1964] PubMed: 37566043
A TGF-β-responsive enhancer regulates SRC expression and epithelial-mesenchymal transition-associated cell migration [ J Cell Sci, 2023, 136(15)jcs261001] PubMed: 37439249
The interactions between integrin α5β1 of liver cancer cells and fibronectin of fibroblasts promote tumor growth and angiogenesis [ Int J Biol Sci, 2022, 18(13):5019-5037] PubMed: 35982891
EGCG Promotes Neurite Outgrowth through the Integrin β1/FAK/p38 Signaling Pathway after Subarachnoid Hemorrhage [ Evid Based Complement Alternat Med, 2021, 2021:8810414] PubMed: 33564320
Integrin α2β1 inhibits MST1 kinase phosphorylation and activates Yes-associated protein oncogenic signaling in hepatocellular carcinoma [ Oncotarget, 2016, 7(47):77683-77695] PubMed: 27765911

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。