GSK215 |
| Catalog No.GC64888 |
GSK215 est un dégradeur puissant et sélectif de la kinase d'adhésion focale PROTAC (FAK) avec un pDC50 de 8,4. GSK215 est conÇu par un liant pour la ligase VHL E3 et l'inhibiteur FAK VS-4718. GSK215 induit une dégradation rapide et prolongée de FAK, donnant un effet durable sur les niveaux de FAK et une déconnexion pharmacocinétique/pharmacodynamique (PK/PD) marquée.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2743427-26-9
Sample solution is provided at 25 µL, 10mM.
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GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect[1].
GSK215 (0.1-1000 nM; 2 hours) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM[1].
GSK215 (8mg/kg; i.h.) treatment shows the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1].
[1]. Law RP, Nunes J, Chung CW, et al. Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs [published online ahead of print, 2021 Aug 20]. Angew Chem Int Ed Engl. 2021;10.1002/anie.202109237.
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