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  3. XPO1-IN-1

XPO1-IN-1 

Cat. No.: HY-144763
Handling Instructions

XPO1-IN-1 (compound D4) is an orally active and potent XPO1 inhibitor, with an IC50 of 24 nM in MM.1S cell. XPO1-IN-1 can efficiently induce cell apoptosis and cell cycle arrest. XPO1-IN-1 displays favorable metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used for multiple myeloma (MM) research.

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

XPO1-IN-1 Chemical Structure

XPO1-IN-1 Chemical Structure

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Description

XPO1-IN-1 (compound D4) is an orally active and potent XPO1 inhibitor, with an IC50 of 24 nM in MM.1S cell. XPO1-IN-1 can efficiently induce cell apoptosis and cell cycle arrest. XPO1-IN-1 displays favorable metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used for multiple myeloma (MM) research[1].

IC50 & Target

XPO1

 

In Vitro

XPO1-IN-1 (compound D4) (24 h) shows high anti-proliferation efficacy in MM.1S cell and lymphomatous cell lines[1].
XPO1-IN-1 (0-10 μM, 24 h) induces cancer cell cycle arrest[1].
XPO1-IN-1 (0-10 μM, 48 h) induces apoptosis of MM.1S cell[1].
XPO1-IN-1 (0-10 μM, 2 h) inhibits XPO1-dependent nuclear export[1].
XPO1-IN-1 shows the good metabolic stability, with more than 80% intact compound remained over rat plasma (2 h), and around 85% intact compound remained in liver microsomes (1 h)[1].

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

Cell Proliferation Assay

Cell Line: MM.1S, Mino, VAL, Rael, Namaiwa, Mutu, H9, JB6, and YT[1]
Concentration:
Incubation Time: 24 h
Result: Showed high anti-proliferation efficacy in MM.1S cell and lymphomatous cell lines (Mino, VAL, Rael, Namaiwa, Mutu, H9, JB6, and YT), with IC50 values of 24, 80.2, 189.1, 201.8, 77.7, 158.2, 101.1, 154.1, and 75.4 nM, respectively.

Cell Cycle Analysis

Cell Line: MM.1S cell[1]
Concentration: 0, 0.1, 1, 5, and 10 μM
Incubation Time: 24 h
Result: Induced cancer cell cycle arrest in high concentration (>100 nM), increased the population of cells arrested in G2 to 37.3% in 5 μM.

Apoptosis Analysis

Cell Line: MM.1S cell[1]
Concentration: 0, 0.1, 1, and 10 μM
Incubation Time: 48 h
Result: Induced apoptosis, significantly increased the apoptotic cell rate to 64.7% (10 μM) when compared to the sample with negative control (6.7%).

Immunofluorescence

Cell Line: MM.1S cell[1]
Concentration: 0, 0.1, 1, and 10 μM
Incubation Time: 2 h
Result: Inhibited XPO1-dependent nuclear export.
In Vivo

XPO1-IN-1 (compound D4) (Sprague Dawley rats; 10 mg/kg, IG; 1 mg/kg, IV; once) shows a good pharmacokinetic properties[1]. Pharmacokinetic Parameters of XPO1-IN-1 in SD rats[1].

Parameters i.g. (10 mg/kg) i.v. (1 mg/kg)
Tmax (h) 2.17 ± 1.76 0.08
T1/2 (h) 2.12 ± 0.16 2.32 ± 0.17
Cmax (ng/mL) 1391.27 ± 586.77 1239.08 ± 152.54
AUC0-t (ng/mL·h) 5774.13 ± 1461.41 1668.03 ± 229.48
AUC0-∞ (ng/mL·h) 6387.17 ± 1637.18 1791.40 ± 236.56
CL (mL/h/kg) 1638.65 ± 431.97 565.30 ± 80.40
F (%) 34.6

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

Animal Model: Sprague Dawley rats[1]
Dosage: 10 mg/kg (IG), 1 mg/kg (IV)
Administration: Oral gavage (IG), IV, once (Pharmacokinetic Analysis)
Result: Showed a good pharmacokinetic properties, with relatively long half-life of 2.12 h (IG) and 2.32 h (IV), respectively, and decent bioavailability F (%) of 34.6%.
Molecular Weight

519.42

Formula

C20H15F6N5O3S

SMILES

CS(=O)(NC1=CC=C(C=C1)/C(C(N)=O)=C\N2C=NC(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=N2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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XPO1-IN-1
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