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 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]
|
||||||||
| 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.
|
||||||||
| 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 |
|
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