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编 号:F753086
分子式:C41H43ClN10O7
分子量:823.3
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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.

体内研究:
FAK PROTAC B5 (Compound B5) possesses favorable plasma stability with the half-life value greater than 289.1 min.

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