产品描述:
PRN-1371 is an irreversible covalent pan-FGFR inhibitor (IC50s = 0.7, 1.3, 4.4, and 19.3 nM for FGFR-1, -2, -3, and -4, respectively).{54899} It is selective for FGFR over VEGFR2 (IC50 = 705 nM) and a panel of 250 kinases (IC50s = >1 µM for all) but does inhibit colony stimulating factor 1 receptor (CSF1R) activity by greater than 90% at 1 µM. PRN-1371 inhibits proliferation in a panel of ten cancer cell lines containing various FGFR mutants (IC50s = 2-231 nM) and induces apoptosis in SNU-16 gastric and RT4 bladder cancer cells (EC50s = 15.9 and 11.8 nM, respectively). It reduces tumor growth in an SNU-16 mouse xenograft model and a patient-derived xenograft (PDX) mouse model of liver cancer when administered at a dose of 15 mg/kg twice per day.