GSK215|cas:2743427-26-9|西域试剂

GSK215,99.85%

产品编号：Bellancom-132296| CAS NO：2743427-26-9| 分子式：C₅₀H₅₉F₃N₁₀O₆S| 分子量：985.13

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货号	价格	库存与货期
Bellancom-132296	￥3072.00	杭州北京（现货）
Bellancom-132296	￥4920.00	杭州北京（现货）
Bellancom-132296	￥9280.00	杭州北京（现货）
Bellancom-132296	￥15000.00	杭州北京（现货）
Bellancom-132296	￥24000.00	杭州北京（现货）

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GSK215

产品介绍

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)。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

GSK215 (8 mg/kg; i.h.; once) degrades FAK, and shows the C_max and t_max values of 526 ng/mL and 0.33 hours, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max and t_max were 526 ng/mL and 0.33 hours, respectively.

体内研究

GSK215 (8 mg/kg; i.h.; once) degrades FAK, and shows the C_max and t_max values of 526 ng/mL and 0.33 hours, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max and t_max were 526 ng/mL and 0.33 hours, respectively.

体内研究

GSK215 (8 mg/kg; i.h.; once) degrades FAK, and shows the C_max and t_max values of 526 ng/mL and 0.33 hours, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max and t_max were 526 ng/mL and 0.33 hours, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (253.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0151 mL	5.0755 mL	10.1509 mL
5 mM	0.2030 mL	1.0151 mL	2.0302 mL
10 mM	0.1015 mL	0.5075 mL	1.0151 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.11 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。