H3B-6527

Description: H3B-6527 is a potent, highly selective, orally bioavailable, covalent FGFR4 inhibitor with IC50 value of ca.1.2 nM. It is at least 250-fold more selective for FGFR4 than for FGFR1-3 (IC50 values of 320, 1, 290 and 1, 060 nM for FGFR1/2/3 respectively). As a FGFR4 inhibitor, H3B-6527 has the potential to be used as an anticancer agent. H3B-6527 acts by specifically binding to and blocking FGFR4 upon administration, which prevents the activation of FGFR4, inhibits FGFR4-mediated signaling and leads to an inhibition of cell proliferation in FGFR4-overexpressing tumor cell.

References: Cancer Res. 2017 Dec 15; 77(24):6999-7013.