GSK215

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GSK215 

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)。

GSK215

GSK215 Chemical Structure

CAS No. : 2743427-26-9

规格 是否有货
5 mg 询价
10 mg 询价
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

生物活性

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].

IC50 & Target

PROTAC; DC50: 1.3 nM (FAK)

体外研究
(In Vitro)

GSK215 (0.1-1000 nM; 2 hours) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0.1-1000 nM
Incubation Time: 2 hours
Result: Increased the FAK degradation.

体内研究
(In Vivo)

GSK215 (8mg/kg; i.h.) treatment shows the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD1 mice (P878/881A)[1]
Dosage: 8 mg/kg
Administration: I.u.(Pharmacokinetic Analysis)
Result: The Cmax and tmax were 526 ng/mL and 0.33 hours, respectively.

分子量

985.13

Formula

C50H59F3N10O6S

CAS 号

2743427-26-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

发表回复