MBM-17S CAS 2083621-91-2

Introduction：Basic information about MBM-17S CAS 2083621-91-2, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

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, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ 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, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ 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