LC-MB12 is an orally active, selective and potent PROTAC FGFR2 complex that degrades FGFR2.LC-MB12 has antiproliferative and antitumor activity.LC-MB12 is used in the study of gastric cancer because of its inhibition of FGFR2 signaling.LC-MB12 has been shown to have antiproliferative and antitumor activity.LC-MB12 has been shown to have antiproliferative and antitumor activity.

NCI-H716 cells:3.2 nM, SNU-16 cells:3.7 nM, FGFR2:11.8 nM (DC50), KATO III cells:29.1 nM

0.5-10000 nM LC-MB12, FGFR2 was degraded in KATO III in a time-dependent manner over 3-12 hours, DC50=11.8 nM. [1]
100 nM LC-MB12 treatment for 6 hours resulted in 77% degradation of FGFR2 in KATO III and 43% degradation in NCI-H1581. [1]
1-10000 nM LC-MB12 treatment for 72 h significantly inhibited the growth of KATO III, SNU-16, and NCI-H716 with IC50=29.1 nM (KATO III), IC50=3.7 nM (SNU-16), and IC50=3.2 nM (NCI-H716), respectively, and induced KATO III G0 /G1 phase block. [1]

Oral administration of 20 mg/kg LC-MB12 was rapidly absorbed in mice (Cmax: 2.6 h) with oral bioavailability (F: 13%). Oral administration for 30 days was well tolerated and showed no significant hepatotoxicity or nephrotoxicity in mice. [1]
20 mg/kg/day LC-MB12 administered orally for 15 days inhibited tumor growth by 63.1% in the SNU-16 nude mouse xenograft model. [1]