MBM-17
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
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- CAS. Nr.: 2083621-90-1
- Formel: C28H28N6O2
- Molecular Weight:480.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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NEK2 3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Bel-7402 | IC50 |
4.53 μM
Compound: 42c; MBM-17
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Cytotoxicity against human Bel7402 cells measured after 72 hrs by MTT assay
Cytotoxicity against human Bel7402 cells measured after 72 hrs by MTT assay
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[PMID: 28039836] |
| HCT-116 | IC50 |
1.06 μM
Compound: 42c; MBM-17
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Cytotoxicity against human HCT116 cells measured after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells measured after 72 hrs by MTT assay
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[PMID: 28039836] |
| MGC-803 | IC50 |
0.48 μM
Compound: 42c; MBM-17
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Cytotoxicity against human MGC803 cells measured after 72 hrs by MTT assay
Cytotoxicity against human MGC803 cells measured after 72 hrs by MTT assay
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[PMID: 28039836] |
MBM-17 (compound 42c) inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.48, 1.06, 4.53 μM, respectively[1].
MBM-17 (0.25-1.0 μM; 24 hours) induced G2/M phase arrest and accumulation of cells with >4N content[1].
MBM-17 (0.5-1.0 μM; 24 hours) triggers apoptosis of cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 and MGC-803 cells
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Concentration:0.25-1.0 μM
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Incubation Time:24 hours
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Result:Obvious accumulation of cells in the G2/M phase with >4 N DNA content.
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Cell Line:HCT-116 and MGC-803 cells
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Concentration:0.5 μM, 1.0 μM
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Incubation Time:24 hours
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Result:For HCT-116 cells, the percentage of total apoptotic cells was 39.3%±3.8% and 47.1%±0.6% at 0.5 μM and 1.0 μM, respectively. For MGC-803 cells, the percentage of total apoptotic cells increased to 32.9%±4.6% and 41.1%±0.2% at 0.25 μM and 0.5 μM, respectively.
MBM-17 (1.0 mg/kg; i.v.) treatment shows CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection; twice a day for 21 days
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Result:Tmor growth was significantly suppressed.
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Animal Model:Male Sprague Dawley (SD) rats[1]
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Dosage:1.0 mg/kg
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Administration:IV injection (Pharmacokinetic Analysis)
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Result:The CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively.
Chemical Information
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CAS. Nr. 2083621-90-1
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Appearance Solid
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Molecular Weight 480.56
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Formel C28H28N6O2
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Color White to off-white
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SMILES
NC(C(C=C1)=C(OCC2=CC=CC=C2)C=C1C3=CN=C4N3C=CC(C5=CN(CCN(C)C)N=C5)=C4)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MBM-17 Related Classifications
HY-101030 Related Classifications
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