| 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 | [Uses]
CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila[1]. | [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). | [in vivo]
CP681301 (1 mM; fed; 10 days) shows anti-tumor activity in 0- to 2-day-old adult Drosophila[1]. | Animal Model: | 0- to 2-day-old adult Drosophila (brat-RNAi tumors)[1] | | Dosage: | 1 mM | | Administration: | Fed, 10 days | | Result: | Reduced active phospho-dCdk5 (Y15) in tumor cells and the self-renewal properties of stem cells, increased the expression of neuronal marker ElaV in these cells and increased the median survival by 2.8-fold. |
| [storage]
4°C, protect from light | [References]
[1] Mukherjee S, et al. CDK5 Inhibition Resolves PKA/cAMP-Independent Activation of CREB1 Signaling in Glioma Stem Cells. Cell Rep. 2018 May 8;23(6):1651-1664. DOI:10.1016/j.celrep.2018.04.016 |
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| Company Name: |
Merck KGaA
|
| Tel: |
(+86) 21 2033 8288 |
| Website: |
http://www.sigmaaldrich.cn |
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