GSK215 是一种有效且具有选择性的 PROTAC 粘着斑激酶 (FAK) 降解剂。GSK215是由VHL E3连接酶粘合剂和FAK抑制剂VS-4718联合设计的。GSK215 诱导 FAK 快速而持久性的降解，对 FAK 水平产生长期影响，并显著降低药代动力学/药效学 (PK/PD)。
货号:ajcx38494
CAS:2743427-26-9
分子式:C50H59F3N10O6S
分子量：985.13
溶解度:DMSO : 250 mg/mL (253.77 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.