FR-027 (FR027)

Chemical Structure : FR-027

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货号: PC-27831Not For Human Use, Lab Use Only.

FR-027 (FR027) is a potent, reversible Exportin 1 (XPO1, CRM1) inhibitor, covalently modifies XPO1 Cys528, inhibits XPO1-NES (nuclear export signal) binding, inhibits XPO1-mediated nuclear export of the SV40NLS-AcGFP-PKINES reporter with IC50 of 54 nM.

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100 mg		Get quote

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生物&药学活性

FR-027 (FR027) is a potent, reversible Exportin 1 (XPO1, CRM1) inhibitor, covalently modifies XPO1 Cys528, inhibits XPO1-NES (nuclear export signal) binding, inhibits XPO1-mediated nuclear export of the SV40NLS-AcGFP-PKINES reporter with IC50 of 54 nM.
targets Cys528 through nucleophilic aromatic substitution.
FR-027 represents a mechan istically distinct class of covalent XPO1 inhibitors that inhibit nuclear export by covalently modifying Cys528 while maintaining the NES binding groove in a closed configuration, thereby preventing ASB8 recruitment and subsequent XPO1 degradation.
FR-027 inhibits XPO1 in a reversible manner.
FR-027 inhibits XPO1-mediated nuclear export with efficacy comparable to selinexor or eltanexor.
FR-027 (2.5 uM) induced pronounced nuclear accumulation of RanBP1 in wild-type Jurkat cells, does not alter the subcellular localization of RanBP1 in XPO1C528S mutant cells.
FR-027 induces potent and XPO1-dependent cytotoxicity acrossa broad panel of tumor cell lines.
FR-027 is orally bioavailable and demonstrates excellent blood brain barrier penetration.
FR-027 (100 mg/kg) significantly delayed tumor growth in orthotopicmurinebraintumormodel by intracranial injection of U87-MG-Luc2 cells into BALB/c nude mice, does not affect platelet, neutrophil, or lymphocyte counts.

物理化学性质&存储条件

分子量	406.24
分子式	C14H8F6N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(3,5-bis(trifluoromethyl)phenyl)-1-(1-methyl-4-nitro-1H-imidazol-5-yl)-1H-1,2,4-triazole

参考文献

1. Van Hauwenhuyse J, et al. Nat Commun. 2026 Jul 22;17(1):8940.

FR-027 (FR027)

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物理化学性质&存储条件

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FR-027 (FR027)

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