产品
编 号：F741748
分子式：C50H59F3N10O6S
分子量：985.13
分子式：C50H59F3N10O6S
分子量：985.13
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2743427-26-9
产品详情
生物活性：
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.
体内研究：
GSK215 (8 mg/kg；ih；一次) 降解 FAK，并显示 Cmax 和 tmax 值分别为 526 ng/mL 和 0.33 小时。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.
体外研究：
GSK215 (0.1-1000 nM；2 小时) 有效地将 FAK 降解增加 >90%，并确定 A549 细胞中的 DC50 为 1.3 nM。 GSK215 诱导的降解依赖于蛋白酶体和泛素。 GSK215 (高于 100 nM，6 小时) 主要减少激酶 CDK7、RPS6KA3、MET 和 GAK。 GSK215 (100 nM，48 小时) 抑制迁移、侵袭和 A549 细胞胶原沉积。
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.
体内研究：
GSK215 (8 mg/kg；ih；一次) 降解 FAK，并显示 Cmax 和 tmax 值分别为 526 ng/mL 和 0.33 小时。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.
体外研究：
GSK215 (0.1-1000 nM；2 小时) 有效地将 FAK 降解增加 >90%，并确定 A549 细胞中的 DC50 为 1.3 nM。 GSK215 诱导的降解依赖于蛋白酶体和泛素。 GSK215 (高于 100 nM，6 小时) 主要减少激酶 CDK7、RPS6KA3、MET 和 GAK。 GSK215 (100 nM，48 小时) 抑制迁移、侵袭和 A549 细胞胶原沉积。
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