DYRKs-IN-1

Names

[ CAS No. ]:
1387090-01-8

[ Name ]:
DYRKs-IN-1

Biological Activity

[Description]:

DYRKs-IN-1 (Example 183) is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-1 has antitumor activity[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK

[Target]

IC50: 9 nM (DYRK1B) and 5 nM (DYRK1A)[2]


[In Vitro]

DYRKs-IN-1 (compound 30) increases the cellular potency against the human colon tumor cell line SW 620 with an EC50 of 27 nM[2].

[References]

[1]. Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1

[2]. 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.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H30ClN7O4

[ Molecular Weight ]:
588.06

Related Compounds