Pyrido[2,3-d]pyrimidine-6-carboxamide, N-[5-[[(3-amino-1-phenylpropyl)amino]carbonyl]-2-chlorophenyl]-7,8-dihydro-2-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-7-oxo-, hydrochloride (1:1)

Biological Activity

DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity[1][2]. DYRKs-IN-1 hydrochloride (compound 30) increases the cellular potency against the human colon tumor cell line SW 620 with an EC50 of 27 nM[1]. DYRKs-IN-1 hydrochloride (Example 183) is a potent DYRKs inhibitor[2].

References

[1]. Anderson K, et al. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. [2]. Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1.