GSK215 |
| Katalog-Nr.GC64888 |
GSK215 ist ein potenter und selektiver Abbauer der fokalen AdhÄsionskinase (FAK) von PROTAC mit einem pDC50 von 8,4. GSK215 wird von einem Binder fÜr die VHL-E3-Ligase und den FAK-Inhibitor VS-4718 entworfen. GSK215 induziert einen schnellen und anhaltenden FAK-Abbau, was zu einer lang anhaltenden Wirkung auf die FAK-Spiegel und einer deutlichen pharmakokinetischen/pharmakodynamischen (PK/PD) Trennung fÜhrt.
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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