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Key Documents

5.32605

Sigma-Aldrich

Aurora A/MYCN Dual Inhibitor, CD532

Sinónimos:

Aurora A/MYCN Dual Inhibitor, CD532, Aurora A Inhibitor, CD532, MYCN Inhibitor, CD532

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About This Item

Fórmula empírica (notación de Hill):
C26H25F3N8O
Número de CAS:
Peso molecular:
522.52
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥97% (HPLC)

Quality Level

form

solid

potency

48 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

tan

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

SMILES string

O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(NC3=NC=CC(NC4=NNC(C5CCCC5)=C4)=N3)C=C2

General description

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 t1/2 = 1.5 h in mice.

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

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Aurora A
Reversible: yes
Secondary Target
MYCN

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

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