Cat. No.: HY-187684

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.

For research use only. We do not sell to patients.

Purity : 99.51%
CAS No.: 3054389-11-3
Formula: C₁₄H₈F₆N₆O₂
Molecular Weight:406.24

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FR-027 Chemical Structure

CAS No.: 3054389-11-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]^[3]

XPO1

54-69 nM (EC₅₀)

In Vitro

Anti-cancerApoptosisOthers

Anti-cancer

FR-027 (0-10 μM; 72 h) potently inhibits proliferation of diverse human cancer cell lines with EC₅₀ values of 0.04-0.28 μM, via selective targeting of XPO1 at Cys₅₂₈^[1].
FR-027 shows in vitro potency matching approved and second-generation XPO1 inhibitors in multiple tumor cell lines, including glioblastoma, and has distinct mechanistic properties: it binds XPO1 via a reversible covalent interaction and does not trigger proteasomal degradation of XPO1^[3].

Anti-cancer

Apoptosis

FR-027 enhances nuclear p53 localization and induces apoptosis in wild-type MOLT-4 human T-ALL cells via selective XPO1 inhibition, with no activity in XPO1^C528S mutant cells^[1].

Others

FR-027 (1-2.5 μM; 15 min preincubation) potently inhibits purified human XPO1 binding to the NES-containing GST-PKINES in vitro at concentrations of 1 μM and 2.5 μM^[1].
FR-027 covalently modifies purified human XPO1 at residue Cys528 via nucleophilic aromatic substitution, forming a 122.9 Da nitro-imidazole adduct^[1].
FR-027 does not induce XPO1 protein degradation in Jurkat, MOLT-4, U87-MG, OCI-LY7, or HAP1 human cancer cell lines^[1].
FR-027 (1-2.5 μM) modified purified human XPO1 does not bind to purified GST-ASB8 in vitro at concentrations of 1 μM and 2.5 μM, due to the closed conformation of the XPO1 NES-binding groove^[1].
FR-027 (33 μM; 1 h incubation) mediated inhibition of purified human XPO1 binding to GST-PKINES is reversible, with partial recovery after 24 hours in inhibitor-free buffer and enhanced reversal with DTT at pH 8.5^[1].
FR-027 (2 h treatment; 24 h post-washout) mediated inhibition of XPO1-dependent nuclear export is reversible in HeLa reporter cells and wild-type Jurkat human T-ALL cells, with substantial recovery of cytoplasmic cargo localization 24 hours post-compound washout^[1].
FR-027 (2 h) potently inhibits XPO1-mediated nuclear export in HeLa reporter cells with an EC₅₀ of 54 nM^[1].
FR-027 selectively targets XPO1 at Cys528 in Jurkat human T-ALL cells, as it fails to induce nuclear accumulation of endogenous RanBP1 in XPO1^C528S mutant cells^[1].
FR-027 reversibly inhibits XPO1 function with an EC₅₀ of 69 nM without inducing XPO1 protein degradation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

diverse panel of human cancer cell lines
Concentration:

0-10 μM
Incubation Time:

72 h
Result:

Reduced tumor cell viability across all tested cell lines with EC50 values ranging from 0.04 to 0.28 μM, matching the potency of selinexor and eltanexor.
Potently inhibited proliferation of wild-type cells but showed no activity in XPO1C528S mutant cells.

In Vivo

Anti-cancerOthers

Anti-cancer

FR-027 (100 mg/kg; p.o.; three times per week) significantly delays tumor growth, prevents leukemic cell dissemination to peripheral tissues, extends overall survival, and delays paralysis in an orthotopic NSG mouse model of T-ALL^[1].
FR-027 (100 mg/kg; p.o.; three times per week; five weeks) delays ascites onset and extends median overall survival to 86 days in an immunocompetent C57BL/6 mouse model of advanced ovarian cancer^[1].
FR-027 (100 mg/kg; p.o.; five times per week) significantly delays tumor growth and extends overall survival in both early and advanced orthotopic BALB/c nude mouse models of glioblastoma^[1].
FR-027 (100 mg/kg; p.o.; five times per week) delays tumor progression, extends overall survival, and prevents intrathecal spinal metastasis in orthotopic BALB/c nude mouse models of PCNSL^[1].

Others

FR-027 (100 mg/kg; p.o.; five times per week; three weeks) demonstrates an improved hematologic safety profile in female CD-1 mice, with no suppression of platelet, lymphocyte, or neutrophil counts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NSG (NOD scid gamma) mice^[1]
Dosage:

100 mg/kg
Administration:

p.o.; three times per week
Result:

Significantly delayed tumor growth as measured by bioluminescence imaging on day 23 after inoculation.
Extended overall survival compared with vehicle controls.
Prevented significant spleen enlargement (spleen size comparable to non-tumor-bearing mice).
Delayed the onset of paralysis due to CNS tumor involvement.

Animal Model:

C57BL/6 mice^[1]
Dosage:

100 mg/kg
Administration:

p.o.; three times per week; five weeks
Result:

Delayed the onset of tumor-induced ascites and first ascites drainage.
Extended median overall survival to 86 days, compared with 58 days for vehicle controls and 73 days for standard-of-care platinum-based alkylating agent plus microtubule-stabilizing taxane treatment.
Was well tolerated with no significant weight loss.

Animal Model:

BALB/c nude mice^[1]
Dosage:

100 mg/kg
Administration:

p.o.; five times per week
Result:

Significantly delayed tumor growth as measured by bioluminescence imaging and magnetic resonance imaging with early treatment, and extended overall survival compared with selinexor and eltanexor.
Substantially reduced tumor growth and nearly doubled median overall survival to 57 days with late treatment (initiated at day 19), compared with 29 days for vehicle controls.

Animal Model:

BALB/c nude mice^[1]
Dosage:

100 mg/kg
Administration:

p.o.; five times per week
Result:

Delayed tumor progression, significantly extended overall survival compared with vehicle control, selinexor, and eltanexor, and prevented spinal metastasis (no increase in spinal tumor signal was observed, and the spinal-to-cranial tumor signal ratio was significantly lower than in vehicle controls by day 23) with early treatment.
Reduced tumor growth and prolonged survival relative to vehicle-treated animals with late treatment (initiated at day 19).

Animal Model:

CD-1 mice (female)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; five times per week; three weeks
Result:

Did not result in weight loss compared with vehicle controls.
Increased platelet counts by up to 24% relative to vehicle controls.
Modestly reduced red blood cell counts by 12%.
Left lymphocyte and neutrophil counts unchanged.

Related Protocols :

Chemical Information

CAS No. 3054389-11-3
Appearance Solid
Molecular Weight 406.24
Formula C₁₄H₈F₆N₆O₂
Color White to off-white
SMILES

CN1C(N(C=N2)N=C2C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=C([N+]([O-])=O)N=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 66.67 mg/mL (164.11 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4616 mL

12.3080 mL

24.6160 mL

5 mM

0.4923 mL

2.4616 mL

4.9232 mL

10 mM

0.2462 mL

1.2308 mL

2.4616 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (298 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Van Hauwenhuyse J, et al. Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy. Nat Commun. 2026.

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4616 mL	12.3080 mL	24.6160 mL	61.5400 mL
	5 mM	0.4923 mL	2.4616 mL	4.9232 mL	12.3080 mL
	10 mM	0.2462 mL	1.2308 mL	2.4616 mL	6.1540 mL
	15 mM	0.1641 mL	0.8205 mL	1.6411 mL	4.1027 mL
	20 mM	0.1231 mL	0.6154 mL	1.2308 mL	3.0770 mL
	25 mM	0.0985 mL	0.4923 mL	0.9846 mL	2.4616 mL
	30 mM	0.0821 mL	0.4103 mL	0.8205 mL	2.0513 mL
	40 mM	0.0615 mL	0.3077 mL	0.6154 mL	1.5385 mL
	50 mM	0.0492 mL	0.2462 mL	0.4923 mL	1.2308 mL
	60 mM	0.0410 mL	0.2051 mL	0.4103 mL	1.0257 mL
	80 mM	0.0308 mL	0.1538 mL	0.3077 mL	0.7692 mL
	100 mM	0.0246 mL	0.1231 mL	0.2462 mL	0.6154 mL

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FR-027