| Identification | Back Directory | [Name]
Benzeneacetamide, N-(5-cyclobutyl-1H-pyrazol-3-yl)-4-(dimethylamino)- | [CAS]
865317-32-4 | [Synonyms]
CP681301
Benzeneacetamide, N-(5-cyclobutyl-1H-pyrazol-3-yl)-4-(dimethylamino)- | [Molecular Formula]
C17H22N4O | [MOL File]
865317-32-4.mol | [Molecular Weight]
298.38 |
| Chemical Properties | Back Directory | [Boiling point ]
585.6±50.0 °C(Predicted) | [density ]
1.251±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : ≥ 100 mg/mL (335.14 mM) | [form ]
Solid | [pka]
13.35±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Biological Activity]
CP-681301 is a potentATP-competitive cyclin-dependent kinase Cdk5 inhibitor (Ki = 13.7 nM; 2.8-/40-fold selectivity over Cdk2/GSK-3β) th at blocks Cdk5 substrates phosphorylation in cultures (tau pS235 IC50 = 513 nM in CHO p25/CDK5/tau transfectants; IC50 ~500 nM against 48-h 10 μM oligomeric Aβ42-stimulated APP pT668 in murine embryonic neurons) and reverses the upregulated tau pS235 level in Cdk5 activator p25-overexpressing transgenic neonatal mice in vivo (5.8 mg/kg s.c.; 6 hrs). CP-681301 selectively inhibits Cdk5-dependent proliferation of human medullary thyroid carcinoma (MTC)but not normal human fibroblasts in cultures (5 μM48 hrs). | [storage]
4°C, protect from light |
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