FAK PROTAC B5

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FAK PROTAC B5 

FAK PROTAC B5 (Compound B5) 是 FAK PROTAC 降解剂，IC50 值为14.9 nM。FAK PROTAC B5 具有很强的 FAK 降解活性，抗增殖活性，血浆稳定性。FAK PROTAC B5 抑制细胞迁移与侵袭。

FAK PROTAC B5

FAK PROTAC B5 Chemical Structure

CAS No. : 2471525-44-5

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生物活性

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].

IC50 & Target

IC50: 14.9 nM (FAK)[1]
体外研究
(In Vitro)

FAK PROTAC B5 (Compound B5) displays strong antiproliferative activity (IC50 = 0.14 ± 0.01 μM) against A549 cells[1].
FAK PROTAC B5 displays excellent FAK degradation activity (86.4% at 10 nM) and the degradation is realized through proteasome degradation pathway[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) has the significant ability to inhibit the migration of A549 cells[1].
FAK PROTAC B5 (0-1.8 μM, 72 h) inhibits the invasion of A549 cells in a concentration-dependent manner[1].
FAK PROTAC B5 exhibits a moderate membrane permeability[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 8 h
Result: Reduced the level of FAK protein in a dose-dependent manner. Displayed excellent FAK degradation activity (86.4% at 10 nM).

Cell Invasion Assay[1]

Cell Line: A549
Concentration: 0.20, 0.60 and 1.80 μM
Incubation Time: 72 h
Result: Significantly reduced the number of A549 cells in a concentration-dependent manner.

体内研究
(In Vivo)

FAK PROTAC B5 (Compound B5) possesses favorable plasma stability with the half-life value greater than 289.1 min[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

823.30

Formula

C41H43ClN10O7
CAS 号

2471525-44-5
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

  • [1]. Yin Sun, et al. Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study. Eur J Med Chem. 2022 Apr 23;237:114373.

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