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Aurora A/MYCN Dual Inhibitor, CD532，10MG，5326050001，Sigma

销售价： ¥ 1700.46 / 件

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订货号： 0BV7210

品牌型号： Sigma 5326050001

货期：询货期

最小订货量： 1件

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商品介绍
规格参数
包装参数

产品介绍 Product Description

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 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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

技术参数 Specifications

assay	≥97% (HPLC)
Quality Segment	100
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
InChI key	GBMIFBVLJSCVJT-UHFFFAOYSA-N

长度(mm)
宽度(mm)
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重量(kg)