3054389-11-3
Chemical Structure
FR-027
- CAS No.: 3054389-11-3
- Formula:C14H8F6N6O2
- Molecular Weight:406.24
InChIKey: JGGIFAXMDNZLJC-UHFFFAOYSA-N
SMILES: CN1C(N(C=N2)N=C2C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=C([N+]([O-])=O)N=C1
Biological Activity: FR-027 is an orally active, blood-brain barrier permeable XPO1 inhibitor with an EC50 value of 54-69 nM in human cells. FR-027 covalently modifies Cys528 of XPO1 via nucleophilic aromatic substitution, maintaining the nuclear export signal binding groove of XPO1 in a closed conformation to block the nuclear export process, and inhibits XPO1 function without inducing its protein degradation. FR-027 promotes cancer cell apoptosis and inhibits the growth of hematological and solid tumor cells. FR-027 can be used in research related to acute lymphoblastic leukemia, ovarian cancer, glioblastoma, and primary central nervous system lymphoma[1][2][3].
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FR-027 | FR-027 is an orally active, blood-brain barrier permeable XPO1 inhibitor with an EC50 value of 54-69 nM in human cells. FR-027 covalently modifies Cys528 of XPO1 via nucleophilic aromatic substitution, maintaining the nuclear export signal binding groove of XPO1 in a closed conformation to block the nuclear export process, and inhibits XPO1 function without inducing its protein degradation. FR-027 promotes cancer cell apoptosis and inhibits the growth of hematological and solid tumor cells. FR-027 can be used in research related to acute lymphoblastic leukemia, ovarian cancer, glioblastoma, and primary central nervous system lymphoma. | |||||||||||||||||||||
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- [1]. Van Hauwenhuyse J, et al. Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy. Nat Commun. 2026.
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[2]. Van Hauwenhuyse J, et al. Abstract 1652: A novel reversible inhibitor of XPO1 with potent efficacy in multiple preclinical mouse models. Cancer Res. 2023;83(7_Supplement):1652.
- [3]. Van Hauwenhuyse J. Identification and development of novel treatment options for glioblastoma [dissertation]. Leuven (Belgium): KU Leuven, Faculty of Medicine; 2026 Jun 26.
Keywords
