Y15

Hersteller MedChem Express
Kategorie Produkte / Inhibitors
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mM*1mL (in Water)
ArtNr HY-12444-10mM
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
FAK inhibitor Y15, Y-15, FAK Inhibitor 14
CAS No.
4506-66-5
Purity
>98%
MW
2840142
Formula
C6H14Cl4N4
Solubility
H2O: >= 59 mg/mL
Biological Description
Y15 is a direct and specific inhibitor of FAK auto-phosphorylation.





IC50 & Target: FAK[1]
In Vitro: Y15 directly blocks autophosphorylation activity of FAK. Y15 inhibits Y397 phosphorylation of FAK starting at 0.1 uM in Panc-1 cells. At a dose of 100 uM, Y15 has the same or better inhibition as TAE226. Of note, total FAK is downregulated at higher doses of Y15. Y15 also blocks phosphorylation of the FAK downstream substrate, paxillin. Total paxillin is decreased at higher doses similar to FAK. Thus, Y15 inhibits FAK phosphorylation in a dose-dependent manner[1]. MTS assay is completed using a range of Y15 doses on all cell lines (TT, K1, BCPAP, and TPC1, respectively).Y15 inhibited cell viability in a dose-dependent manner across all thyroid cell lines evaluated. IC50 is 2.05, 5.74, 9.99, and 17.54 uM for TT, TPC1, BCPAP, and K1, respectively[2].
In Vivo: Nude mice bearing Panc si-ctrl xenografts are treated with TAE226, a dual FAK and IGF-1R tyrosine kinase inhibitor, to provide a reference for the antitumor effect of dual inhibition of FAK and IGF-1R. Without drug treatment, Panc si5-IGF-1R xenografts grew slower than Panc si-ctrl xenografts (Panc si5-IGF-1R/PBS vs. Panc si-ctrl/PBS), suggesting moderate tumor suppression by inhibiting the IGF-1R pathway only. Further inhibition of FAK activity by Y15 treatment suppresses the growth of Panc si5-IGF-1R xenografts more drastically (Panc si5-IGF-1R/PBS vs. Panc si5-IGF-1R/Y15). A similar antitumor effect is seen in Panc si-ctrl xenografts treated with TAE226 (Panc si5-IGF-1R/Y15 vs. Panc si-ctrl/TAE226). Mice demonstrates normal grooming and eating habits throughout the experiment[3].
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 10mM*1mL (in Water)
Lieferbar: In stock
Listenpreis: 114,29 €
Preis: 114,29 €
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