N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine

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N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine Basic information
Product Name:N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine
Synonyms:N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine;N,N-Dimethyl-4-(pyrazolo[1,5-b]pyridazin-3-yl)pyrimidin-2-amine;DYRK1A inhibitor compound 11
CAS:2814486-79-6
MF:C12H12N6
MW:240.26
EINECS:
Product Categories:
Mol File:2814486-79-6.mol
N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine Structure
N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine Chemical Properties
density 1.34±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
solubility DMSO: Slightly soluble: 1-10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml
pka3.04±0.10(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine Usage And Synthesis
UsesDYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe[1].
in vivo

DYRK1-IN-1 (1 mg/kg; i.v.) shows high clearance[1].

Animal Model:SpragueDawley rats[1]
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:I.v.
Result:High clearance was observed.
IC 50DYRK1A: 220 nM (IC50); DYRK1A: 3 nM (Kd); DYRK1B: 56 nM (Kd)
References[1] Henderson SH, et al. Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. J Med Chem. 2021;64(15):11709-11728. DOI:10.1021/acs.jmedchem.1c01115
N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine Preparation Products And Raw materials
Tag:N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine(2814486-79-6) Related Product Information
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