LC-MB12 (20 mg/kg/day, p.o., 15 days) inhibits tumor growth to 63.1% in SNU-16 xenograft models of nude mice[1].
LC-MB12 (20 mg/kg, p.o.) shows fast absorption (Cmax: 2.6 h) and orally bioavailable (F: 13%) in mice[1].
LC-MB12 (20 mg/kg, p.o., 30 days) is well tolerated and has no apparent hepatotoxicity or nephrotoxicity in mice[1].
In Vivo PK Properties of LC-MB12[1]
| parameter | T1/2 | Tmax (ng?h/mL) | Cmax | AUC(0-∞)1/2 | Vss (h) | CL | F |
| unit | h | h | ng/mL | h*ng/mL | mL/kg | mL/h/kg | % |
| iv (3 mg/kg) | 0.97 | 0.083 | 655.29 | 421.61 | 6233.19 | 7289.12 | / |
| po (20 mg/kg) | 1.47 | 2.67 | 82.07 | 387.27 | / | / | 13.07 |
| Animal Model: | SNU-16 xenografted in BALB/c-nu mice[1]. |
| Dosage: | 20 mg/kg/day |
| Administration: | oral administration (p.o.) 15 days |
| Result: | Achieved 63.1% tumor growth inhibition innocuously.
Inhibited FGFR phosphorylation and total FGFR2 protein and decreased phosphorylation levels of downstream pPLCγ and ERK1/2.
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