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FAK degrader F2

Chemical Structure : FAK degrader F2

CAS No.:

FAK degrader F2 (FAK PROTAC F2)

Catalog No.: PC-22493Not For Human Use, Lab Use Only.

FAK PROTAC F2 is a potent, selective FAK CRBN-recruiting PROTAC degrader based on the FAK inhibitor Ifebemtinib (IN10018) with DC50 of 27.72 nM and 60.10 nM for total FAK and phosphorylated FAK in MDA-MB-231 cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

FAK PROTAC F2 is a potent, selective FAK CRBN-recruiting PROTAC degrader based on the FAK inhibitor Ifebemtinib (IN10018) with DC50 of 27.72 nM and 60.10 nM for total FAK and phosphorylated FAK in MDA-MB-231 cells.
FAK PROTAC F2 exhibits potent inhibitory activities against 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435 cells with IC50 values of 0.73, 1.09, 5.84 and 3.05 μM, respectively.
FAK PROTAC F2 also remarkably reversed the multidrug resistance (MDR) in HCT8/T, A549/T and MCF-7/ADR cells.
FAK PROTAC F2 exerts anti-tumor effects by inhibiting AKT and ERK signaling pathways and affecting EMT (epithelial-mesenchymal transition).
FAK PROTAC F2 reverses the resistance of multidrug-resistant tumor cells to chemotherapy drugs in vitro and in vivo.

Physicochemical Properties

M.Wt 926.93
Formula C47H46F4N8O8
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(1-((1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-inden-5-yl)piperidin-4-yl)methyl)piperidin-4-yl)-2-fluoro-5-methoxy-4-((4-((2-methyl-3-oxoisoindolin-4-yl)oxy)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide

References

1. Xu MS, et al. Acta Pharmacol Sin. 2024 Jun 6. doi: 10.1038/s41401-024-01312-w.

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