GSK215

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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)。

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.

Western Blot Analysis Cell Line:A549 cells Concentration:0.1-1000 nM Incubation Time:2 h Result:Increased the FAK degradation.Cell Migration Assay Cell Line:A549 cells Concentration:100 nM Incubation Time:48 h Result:Inhibited cell migration.Cell Invasion Assay Cell Line:A549 cells Concentration:100 nM Incubation Time:48 h Result:Inhibited cell invasion.

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.

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Angiogenesis

FAK

FAK | PROTACs

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2743427-26-9

985.13

C50H59F3N10O6S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (253.77 mM; 超声助溶 )

CNC(=O)c1ccccc1Nc1cc(Nc2ccc(cc2OC)N2CCN(CC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(cc3)-c3scnc3C)C(C)(C)C)CC2)ncc1C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years