FR-027 | Reversible XPO1 inhibitor

CAS:
 3054389-11-3
Catalog Number:
 10-3986
FR-027 chemical structure

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FR-027 (3054389-11-3) is a novel inhibitor of Exportin 1 (XPO1/CRM1). Unlike other XPO1 inhibitors, it reacts with Cys528 through nucleophilic aromatic substitution instead of Michael addition, does not induce degradation of XPO1, and reversibly inhibits XPO1-mediated nuclear export.  FR-027 displays EC50s <1 µM against multiple solid and hematological tumor cell lines.   It is active in vivo, increasing overall survival rates in MOLT-4 T-ALL xenograft, syngeneic ID8-fLuc ovarian cancer, and xenograft brain tumor mouse models without inducing thrombocytopenia, lymphopenia, or neutropenia.

References/Citations:

  1. Van Hauwenhuyse et al. (2026), Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy; Nat. Commun. 17 8940
3054389-11-3, CRM1 inhibitor, Exportin 1 inhibitor, FR-027, FR-027 supplier, reversible XPO1 inhibitor, XPO1 inhibitor
CAS:
3054389-11-3
Catalog Number:
10-3986
Activity:
XPO1 inhibitor
Chemical Names:
3-(3,5-bis(Trifluoromethyl)phenyl)-1-(1-methyl-4-nitro-1H-imidazol-5-yl)-1H-1,2,4-triazole
Molecular Weight:
406.25
Molecular Formula:

C14H18F6N6O2

Solubility:
Soluble in DMSO (60 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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FR-027 (3054389-11-3) is a novel inhibitor of Exportin 1 (XPO1/CRM1). Unlike other XPO1 inhibitors, it reacts with Cys528 through nucleophilic aromatic substitution instead of Michael addition, does not induce degradation of XPO1, and reversibly inhibits XPO1-mediated nuclear export.  FR-027 displays EC50s <1 µM against multiple solid and hematological tumor cell lines.   It is active in vivo, increasing overall survival rates in MOLT-4 T-ALL xenograft, syngeneic ID8-fLuc ovarian cancer, and xenograft brain tumor mouse models without inducing thrombocytopenia, lymphopenia, or neutropenia.

References/Citations:

  1. Van Hauwenhuyse et al. (2026), Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy; Nat. Commun. 17 8940

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