| Identification | Back Directory | [Name]
MBM-55 | [CAS]
2083622-09-5 | [Synonyms]
MBM-55
Inhibitor,arrest,proliferation,antitumor,Apoptosis,cycle,cell,MBM 55,selectivity,inhibit,MBM-55,Nek2,MBM55
Benzamide, 4-[7-[1-[2-(dimethylamino)ethyl]-1H-pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[(3-fluorophenyl)methoxy]- | [Molecular Formula]
C28H27FN6O2 | [MDL Number]
MFCD32174237 | [MOL File]
2083622-09-5.mol | [Molecular Weight]
498.55 |
| Chemical Properties | Back Directory | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
15.40±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 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-55 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]. | [in vivo]
MBM-55 (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-55 (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. | 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 ng/h/mL, respectively.
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| [IC 50]
NEK2: 1 nM (IC50) | [storage]
Store at -20°C | [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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