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|---|---|---|
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| Cat. No. : | HY-101030 |
| M.Wt: | 480.56 |
| Formula: | C28H28N6O2 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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].
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].
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