Y15

Catalog No.S5321 Batch:S532101

Technical Data

Formula	C₆H₁₀N₄.4HCl
Molecular Weight	284.01	CAS No.	4506-66-5
Solubility (25°C)*	In vitro	DMSO	56 mg/mL (197.17 mM)
		Water	56 mg/mL (197.17 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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.

Targets

FAK ^[1]
(Cell-free assay)

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 t_1/2 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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines The thyroid cancer cell lines: TPC1, TT and BCPAP Concentrations 0-50 μM Incubation Time 24 h Method 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.
Animal Study:^{^[3]}	Animal Models The CD-1 albino mice; 7 weeks old (males) and 9 weeks old (females) Dosages 30 mg/kg or 100 mg/kg Administration intraperitoneal (IP) or oral (PO) delivery

Cell Assay:^{^[1]}

Cell lines
The thyroid cancer cell lines: TPC1, TT and BCPAP
Concentrations
0-50 μM
Incubation Time
24 h
Method
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.

Animal Study:^{^[3]}

Animal Models
The CD-1 albino mice; 7 weeks old (males) and 9 weeks old (females)
Dosages
30 mg/kg or 100 mg/kg
Administration
intraperitoneal (IP) or oral (PO) delivery

References

Selleck's Y15 has been cited by 5 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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