GSK215 |
| رقم الكتالوجGC64888 |
GSK215 عبارة عن مطهر كيناز التصاق بؤري انتقائي من PROTAC مع pDC50 يبلغ 8.4تم تصميم GSK215 بواسطة رابط لـ VHL E3 ligase ومثبط FAK VS-4718يحث GSK215 على تحلل FAK سريعًا وطويل الأمد ، مما يعطي تأثيرًا طويل الأمد على مستويات FAK وفصل الحرائك الدوائية / الديناميكيات الدوائية (PK / PD) بشكل ملحوظ
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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