THZ1 is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM, also weakly inhibits CDK12 with IC50 of 250 nM.
THZ1 displays broad-based activity a subset of cancer cell lines with IC50s of <200 nM.
THZ1 causes decreased cellular proliferation and an increase in apoptotic index (MCL-1, XIAP), disproportionally affects transcription of RUNX1 in Jurkat T-ALL cells.
THZ1 demonstrates efficacy against primary leukemia cells and in a bioluminescent xenografted model at 10mg/kg.
