| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
MBM-55S (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule in nude mice bearing HCT-116 xenografts[1].
MBM-55S (1.0 mg/kg; i.v.) treatment shows the CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 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: | Significantly suppressed tumor growth. |
| 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 were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ml/min/kg, respectively. |
| [IC 50]
RSK1: 5.4 nM (IC50); NEK2: 1 nM (IC50); DYRK1A: 6.5 nM (IC50) | [References]
[1] Xi JB, et al. Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. Eur J Med Chem. 2017 Jan 27;126:1083-1106. DOI:10.1016/j.ejmech.2016.12.026 |
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