662163-81-7
662163-81-7 structure
- Name: Importazole
- Chemical Name: N-(1-Phenylethyl)-2-(1-pyrrolidinyl)-4-quinazolinamine
- CAS Number: 662163-81-7
- Molecular Formula: C20H22N4
- Molecular Weight: 318.415
- Catalog: Research Areas Cancer
- Create Date: 2018-02-19 21:01:58
- Modify Date: 2025-08-25 14:10:13
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Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
| Name | N-(1-Phenylethyl)-2-(1-pyrrolidinyl)-4-quinazolinamine |
|---|---|
| Synonyms |
N-(1-Phenylethyl)-2-(1-pyrrolidinyl)-4-quinazolinamine
4-Quinazolinamine, N-(1-phenylethyl)-2-(1-pyrrolidinyl)- Importazole |
| Description | Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β. |
|---|---|
| Related Catalog | |
| In Vitro | Importazole specifically blocks importin-β-mediated nuclear import both in Xenopus egg extracts and cultured cells, without disrupting transportin-mediated nuclear import or CRM1-mediated nuclear export. Importazole impairs the release of an importin-β cargo FRET probe and causes both predicted and novel defects in spindle assembly[1]. Importazole displays an IC50 of approximately 15 μM for inhibition of NFAT-GFP import. Importazole has an IC50 of approximately 22.5 μM in HeLa cells following treatment over a 24-hour period[1]. Importazole induces a dose-and time-dependent inhibition of myeloma cells growth. And the IC50 values of importazole on RPMI 8226 and NCI-H929 after 48 hours incubation are (4.43±0.41) and (4.78±0.35) μmol/L, respectively. Treatment of RPMI 8226 and NCI-H929 cells with 8 μmol/L importazole for 24 h could inhibit NF-κB import to nucleus and reduce its DNA binding activity[2]. |
| Cell Assay | HEK 293 cells stably expressing NFAT-GFP are grown on glass coverslips to approximately 50% confluency prior to drug treatment. In all cases, importazole is used at 40 μM and leptomycin B is used at 10 ng/mL. For controls, DMSO is used at a concentration of 0.4%. Ionomycin is added at 1.25 μM. Importazole and leptomycin B treatments are all for 1 hour. In all experiments cells are fixed with 4% formaldehyde prior to fluorescence microscopy. DNA is visualized with 1 μg/mL Hoechst dye. For quantification, 100 cells from each condition are analyzed and the percentage that shows nuclear accumulation of NFAT-GFP are calculated[1]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 516.8±42.0 °C at 760 mmHg |
| Molecular Formula | C20H22N4 |
| Molecular Weight | 318.415 |
| Flash Point | 266.3±27.9 °C |
| Exact Mass | 318.184448 |
| LogP | 3.30 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.682 |
| Storage condition | -20℃ |
| RIDADR | NONH for all modes of transport |
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