Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (2R,3S)-3-[[6-[[(4,6-dimethyl-3-pyridinyl)methyl]amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-2-pentanol
Purity: ≥98%
Formula Markup: C21H31N7O
Formula Weight: 397.51742
CAS Number: 1070790-89-4
Notes: Fadraciclib is an inhibitor of cyclin-dependent kinase 2 (Cdk2) and Cdk9 (IC50s = 4.5 and 20.5 nM, respectively).{65351} It is selective for Cdk2 and Cdk9 over Cdk1, -4, and -7 (IC50s = 278, 193, and 232 nM, respectively). Fadraciclib inhibits the proliferation of COLO 205 cells (IC50 = 0.31 µM), as well as inhibits proliferation in a panel of five breast cancer cell lines (IC50s = <0.4 µM for all). It decreases phosphorylation of the RNA polymerase II C-terminal domain and RB, Cdk9 and Cdk2 targets, respectively, and induces apoptosis in COLO 205 cells. Fadraciclib (40 and 55 mg/kg) reduces tumor volume in an EoL-1 eosinophilic leukemia mouse xenograft model. It also inhibits tumor growth in an HL-60 mouse xenograft model when administered at a dose of 70 mg/kg.
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