| Identification | Back Directory | [Name]
N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine | [CAS]
2814486-79-6 | [Synonyms]
N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine | [Molecular Formula]
C12H12N6 | [MOL File]
2814486-79-6.mol | [Molecular Weight]
240.26 |
| Chemical Properties | Back Directory | [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 | [form ]
Solid | [pka]
3.04±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
DYRK1-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: | Sprague?Dawley rats[1] | | Dosage: | 1 mg/kg (Pharmacokinetic Analysis) | | Administration: | I.v. | | Result: | High clearance was observed.
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| [IC 50]
DYRK1A: 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 |
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