Formulation: A solid
Formal Name: (1S,3S)-N1-[5-(1-ethylpropyl)pyrazolo[1,5-a]pyrimidin-7-yl]-1,3-cyclopentanediamine, monohydrochloride
Purity: ≥95%
Formula Markup: C16H25N5 • HCl
Formula Weight: 323,9
Shelf life (days): 1460
Notes: KB-0742 is an inhibitor of cyclin-dependent kinase 9 (Cdk9; IC50 = 6 nM).{66711} It is selective for Cdk9 over Cdk1-8 (IC50s = 397->10,000 nM) and Cdk12-19 (IC50s = 372->10,000 nM). KB-0742 (0.64-7.73 µM) induces cell cycle arrest at the G1 phase and apoptosis in BT-20, BT-549, MDA-MB-231, MT-3, and Hs 578T triple-negative breast cancer (TNBC) cells. In vivo, KB-0742 (60 mg/kg) reduces tumor volume in the MYC-amplified CTG-0437 patient-derived xenograft (PDX) mouse model of TNBC.