Synonyms: 1-[4-(2-Aminopyrimidin-4-yloxy)phenyl]-3-[4-[(4-methylpiperazin-1-yl)methyl]-3-trifluoromethylphenyl]urea; AUZ 454; AUZ-454; AUZ454; CCG 269702; CCG-269702; CCG269702; K 03861; K-03861; N-[4-[(2-Amino-4-pyrimidinyl)oxy]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]urea
Molecular Formula: C24H26F3N7O2
Molecular Weight: 501.5
Linear Structural Formula: C24H26F3N7O2
MDL Number: MFCD19443769
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: K03861 is an ATP site-binding, cyclin-competitive, type II CDK2 inhibitor that selectively targets and locks the kinase in its inactive DFG-out conformation (CDK2 Kd = 50 nM, DFG-out stabilizing CDK2-C118L/A144C mutant Kd = 9.7 nM without vs. 134.1 nM with bound cycB; CDK2-C118L/A144C-cycA IC50 = 0.8 muM), rendering it incompatible for cyclin bining. K03861 selectively inhibits CDK2-C118L/A144C over CycA-bound wt CDK2 by in vitro kinase assay (IC50 = 0.8 vs. >10 muM) and inhibits the proliferation of immortalized multipotent otic progenitor (iMOP) murine cell line (by 81% and 92%, resepectively, at 0.1 and 1.0 muM).