ChemicalBook CAS DataBase List 865317-32-4

865317-32-4

Name	Benzeneacetamide, N-(5-cyclobutyl-1H-pyrazol-3-yl)-4-(dimethylamino)-
CAS	865317-32-4
Molecular Formula	C17H22N4O
Molecular Weight	298.38
MOL File	865317-32-4.mol

Chemical Properties

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

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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