Catalog No.: PC-73407Not For Human Use, Lab Use Only.
Bezuclastinib (CGT9486, PLX9486) is a potent, selective tyrosine kinase inhibitor (TKI) targeting mutated KIT and demonstrating potent activity in vitro against primary exon 9 and 11 mutations, as well as secondary exon 17 and 18 mutations.
Bezuclastinib (CGT9486, PLX9486) is a potent, selective tyrosine kinase inhibitor (TKI) targeting mutated KIT and demonstrating potent activity in vitro against primary exon 9 and 11 mutations, as well as secondary exon 17 and 18 mutations.
Bezuclastinib (CGT9486, PLX9486) is a potent inhibitor of growth and KIT phosphorylation in the imatinib-sensitive and imatinib-resistant BaF3 cell lines, with growth IC50=61 nM for KIT-WT and more potently against BaF3 KIT p.D816V (IC50=6.6 nM) and BaF3 KIT p.V560G/D816V (IC50=7.1 nM).
Bezuclastinib (CGT9486, PLX9486) demonstrated signifcant tumor regression and strong inhibition of MAPK activation in imatinib-resistant GIST patient-derived xenograft (PDX) models.
