5.32605

Aurora A/MYCN Dual Inhibitor, CD532

• Synonyme(s) : Aurora A/MYCN Dual Inhibitor, CD532, Aurora A Inhibitor, CD532, MYCN Inhibitor, CD532
• Formule empirique (notation de Hill): C₂₆H₂₅F₃N₈O
• Numéro CAS: 1639009-81-6
• Poids moléculaire : 522.52
• Numéro MDL: MFCD32671941
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 48 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: tan
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(NC3=NC=CC(NC4=NNC(C5CCCC5)=C4)=N3)C=C2

Description

Description générale

A cell permeable diaminopyrimidine derived compound that acts as a highly potent and selective inhibitor of Aurora A (IC₅₀ = 48 nM). Acts by binding to the hinge region via a pyrazole moiety and stabilizes a DFG-in, inactive conformation of Aurora A. Potentiates the loss of the wild-type MYCN protein by disrupting MYCN-Aurora A complex and allowing its ubiquitination and proteasomal degradation in MYCN-amplified SK-N-BE (2) and Kelly neuroblastoma cells (EC₅₀ = 223 and 146.7 nM, respectively). Causes a loss of S-phase entry of cells and allows their accumulation in both G0/G1 and G2 phases. Shown to be effective in vivo with serum t1/2 = 1.5 h in mice.

A cell permeable diaminopyrimidine derived compound that acts as a highly potent and selective inhibitor of Aurora A (IC₅₀ = 48 nM). Acts by binding to the hinge region via a pyrazole moiety and stabilizes a DFG-in, inactive conformation of Aurora A. Potentiates the loss of the wild-type MYCN protein by disrupting MYCN-Aurora A complex and allowing its ubiquitination and proteasomal degradation in MYCN-amplified SK-N-BE (2) and Kelly neuroblastoma cells (EC₅₀ = 223 and 146.7 nM, respectively). Causes a loss of S-phase entry of cells and allows their accumulation in both G0/G1 and G2 phases. Shown to be effective in vivo with serum t_1/2 = 1.5 h in mice.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Aurora A

Reversible: yes

Secondary Target
MYCN

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Lee, J.K., et al. 2016. Cancer Cell.29, In press.
Gustafson, W. C., et al. 2014. Cancer Cell.26, 414.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable