| CAS NO: | 2743427-26-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 2743427-26-9 |
| 分子式 | C50H59F3N10O6S |
| 分子量 | 985.13 |
| 溶解度 | DMSO : 250 mg/mL (253.77 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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