1. Apoptosis
  2. Apoptosis
  3. MBM-17

MBM-17 

Cat. No.: HY-101030
Handling Instructions

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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MBM-17 Chemical Structure

MBM-17 Chemical Structure

CAS No. : 2083621-90-1

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Description

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[1].

IC50 & Target

IC50: 3 nM (Nek2), 5800 nM (Aurora A)[1]

In Vitro

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].

Cell Cycle Analysis[1]

Cell Line: HCT-116 and MGC-803 cells
Concentration: 0.25-1.0 μM
Incubation Time: 24 hours
Result: Obvious accumulation of cells in the G2/M phase with >4 N DNA content.

Apoptosis Analysis[1]

Cell Line: HCT-116 and MGC-803 cells
Concentration: 0.5 μM, 1.0 μM
Incubation Time: 24 hours
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.
In Vivo

MBM-17 (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule[1].
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].

Animal Model: Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; twice a day for 21 days
Result: Tmor growth was significantly suppressed.
Animal Model: Male Sprague Dawley (SD) rats[1]
Dosage: 1.0 mg/kg
Administration: IV injection (Pharmacokinetic Analysis)
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.
Molecular Weight

480.56

Formula

C₂₈H₂₈N₆O₂

CAS No.

2083621-90-1

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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Storage

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

References
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Keywords:

MBM-17MBM17MBM 17ApoptosisantitumorselectivityNek2proliferationcellcyclearrestapoptosisInhibitorinhibitorinhibit

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MBM-17
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