货号	规格	价格	上海	北京	武汉	南京	购买数量
S23210-5mg	98%	￥7500.00 S23210-5mg ￥7500.00 2-3天	0 货期：2-3天	-	-	-
S23210-10mg	98%	￥12000.00 S23210-10mg ￥12000.00 2-3天	0 货期：2-3天	-	-	-

产品介绍

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

产品描述：

靶点：

PROTAC; pDC50: 8.4 (FAK);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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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GSK215