Y15

Catalog No.S5321 Synonyms: 1,2,4,5-Benzenetetraamine tetrahydrochloride

Y15 Chemical Structure

Molecular Weight(MW): 284.01

Y15 is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.

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Biological Activity

Description Y15 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 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].

Protocol

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: The CD-1 albino mice; 7 weeks old (males) and 9 weeks old (females)
  • Formulation: dissolved in 1×PBS for pharmacokinetics study or sterile water for PO delivery in toxicity study
  • Dosages: 30 mg/kg or 100 mg/kg
  • Administration: intraperitoneal (IP) or oral (PO) delivery
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 56 mg/mL (197.17 mM)
Water 56 mg/mL (197.17 mM)
Ethanol 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.

Chemical Information

Molecular Weight 284.01
Formula

C6H10N4.4HCl

CAS No. 4506-66-5
Storage powder
in solvent
Synonyms 1,2,4,5-Benzenetetraamine tetrahydrochloride

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID