Dual BET-Kinase inhibitor 3 is a potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.
Dual BET-Kinase inhibitor 3 is a potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.
Dual BET-Kinase inhibitor 3 also significantly inhibits NTRK3 (IC50=5 nM), ROS1 (IC50=11 nM), PDGFRβ (IC50=16 nM) and FGFR1 (IC50=43 nM).
Dual BET-Kinase inhibitor 3 shows equal activity against the first and second bromodomains of BRD4 and shows only slightly reduced activity against BRDT-1.
Dual BET-Kinase inhibitor 3 inhibits cell growth of MM and AML cell lines with IC50 of <1 uM, reduces c-MYC and p-STAT3 levels and induces G1 arrest, display differential activity across cancer cell lineages.
