DYRKs-IN-1 hydrochloride

• CAT Number: I044330
• CAS Number: 1386980-55-7
• Molecular Formula: C30H31Cl2N7O4
• Molecular Weight: 624.52
• Purity: ≥95%
• Synonyms: N-[5-[(3-amino-1-phenylpropyl)carbamoyl]-2-chlorophenyl]-2-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-7-oxo-8H-pyrido[2,3-d]pyrimidine-6-carboxamide;hydrochloride
• InChI: InChI=1S/C30H30ClN7O4.ClH/c31-23-9-6-18(27(39)34-24(10-11-32)17-4-2-1-3-5-17)13-25(23)35-28(40)22-12-19-14-33-30(37-26(19)36-29(22)41)38-15-20-7-8-21(16-38)42-20;/h1-6,9,12-14,20-21,24H,7-8,10-11,15-16,32H2,(H,34,39)(H,35,40)(H,33,36,37,41);1H
• InChIKey: XLHHYTUBPOMTDK-UHFFFAOYSA-N
• SMILES: C1CC2CN(CC1O2)C3=NC=C4C=C(C(=O)NC4=N3)C(=O)NC5=C(C=CC(=C5)C(=O)NC(CCN)C6=CC=CC=C6)Cl.Cl

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].

Reference

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