MBM-17S
MBM-17S Basic information
- Product Name:
- MBM-17S
- Synonyms:
-
- MBM-17S
- MBM17S,MBM 17S
- CAS:
- 2083621-91-2
- MF:
- C32H34N6O6
- MW:
- 598.66
- Mol File:
- 2083621-91-2.mol
MBM-17S Usage And Synthesis
Description
MBM-17S s a potent NIMA-related kinase 2 (Nek2) inhibitor. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
Uses
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice[1].
in vivo
MBM-17S (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule[1].
MBM-17S (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. |
IC 50
NEK2: 3 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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