MBM-55S
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
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- CAS No.: 2083624-07-9
- Formule: C36H39FN6O10
- Masse moléculaire:734.73
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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RSK1 5.4 nM (IC50) |
NEK2 1 nM (IC50) |
DYRK1A 6.5 nM (IC50) |
MBM-55S inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively[1].
MBM-55S (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells[1].
MBM-55S (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 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 cells
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Concentration:0.5, 1 μM
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Incubation Time:24 hours
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Result:Induced G2/M phase arrest and accumulation of cells with >4N content.
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Cell Line:HCT-116 cells
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Concentration:0.5, 1 μM
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Incubation Time:24 hours
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Result:Caused cell apoptosis in a concentration-dependent manner.
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:Significantly suppressed tumor growth.
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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 were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ml/min/kg, respectively.
Chemical Information
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CAS No. 2083624-07-9
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Masse moléculaire 734.73
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Formule C36H39FN6O10
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SMILES
NC(C(C=C1)=C(OCC2=CC=CC(F)=C2)C=C1C3=CN=C4N3C=CC(C5=CN(CCN(C)C)N=C5)=C4)=O.O=C(O)CCC(O)=O.O=C(O)CCC(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MBM-55S Related Classifications
HY-101029A Related Classifications
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