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
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M.Wt
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926.93
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Formula
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C47H46F4N8O8
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Xu MS, et al. Acta Pharmacol Sin. 2024 Jun 6. doi: 10.1038/s41401-024-01312-w.
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