- 产品描述： GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. 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
- 靶点： PROTAC; pDC50: 8.4 (FAK)
- 体外研究： GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM in A549 cells.
GSK215 induced degradation is proteasome and ubiquitin dependent.
GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK[.
GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells.
- 体内研究： GSK215 (8 mg/kg; i.h.; once) degrades FAK, and shows the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively. Animal Model: Male CD1 mice (P878/881A), 7-9 weeks Dosage: 8 mg/kg Administration: Single subcutaneous injection Result: Caused a rapid and profound degradation of FAK in liver over time, with a maximal degradation of ~85% being achieved within 18 h. Endogenous FAK was found to still be reduced by ~60% at 96 h post-dose.The Cmax and tmax were 526 ng/mL and 0.33 hours, respectively.
- 参考文献：
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.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 备注： GSK215 是一种有效且具有选择性的 PROTAC 粘着斑激酶 (FAK) 降解剂，pDC50 值为 8.4。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)。
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.015 ml 5.075 ml 10.151 ml 5 mM 0.203 ml 1.015 ml 2.03 ml 10 mM 0.102 ml 0.508 ml 1.015 ml 50 mM 0.02 ml 0.102 ml 0.203 ml
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