Y15

製品コードS5321 バッチS532101

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 DMSO 56 mg/mL (197.17 mM)
Water 56 mg/mL (197.17 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/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 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, this compound inhibits pY397 and total FAK expression in a dose-dependent manner. It causes effective dose-dependent detachment in all thyroid cancer cell lines. This chemical 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]. It 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, this compound is very rapidly absorbed in mice, reaching maximum plasma concentration in 4.8 min. It 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 this chemical by oral administration is 200 mg/kg, and the multiple maximum tolerated dose is 100 mg/kg by PO during 7 day study. It 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 this compound 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

参考

  • https://pubmed.ncbi.nlm.nih.gov/25277206/
  • https://academic.oup.com/carcin/article/33/5/1004/2463779
  • https://pubmed.ncbi.nlm.nih.gov/24915938/

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：

Activation of integrin signaling up-regulates pro-inflammatory cytokines in JAK2-V617F positive hematopoietic cells [ Cell Commun Signal, 2025, 23(1):368] PubMed: 40790213
Phillygenin Improves the Focal Adhesion Kinase/Glycogen Synthase Kinase 3β/β-Catenin Axis to Promote Mesenchymal Stem Cell Osteogenic Differentiation [ Phytother Res, 2025, 10.1002/ptr.8519] PubMed: 40828205
Acoustic modulation of mechanosensitive genes and adipocyte differentiation [ Commun Biol, 2025, 8(1):595] PubMed: 40240542
In vitro synergistic effect of AXL, FAK and ErbB receptors inhibitors for head and neck cancer [ Biol Direct, 2025, 20(1):77] PubMed: 40605022
Signaling pathways of pro-IL-1β production induced by mechanical stress in gingival epithelial cells [ J Oral Biosci, 2025, S1349-0079(25)00015-5] PubMed: 39921162
β1 Integrin/FAK signaling regulates interleukin-8 production in human gingival epithelial Ca9-22 cells [ J Oral Biosci, 2025, S1349-0079(25)00004-0] PubMed: 39826873
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
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

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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