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Merck

189406

Aurora Kinase/Cdk Inhibitor

The Aurora Kinase/Cdk Inhibitor, also referenced under CAS 443797-96-4, controls the biological activity of Aurora Kinase/Cdk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

別名:

Aurora Kinase/Cdk Inhibitor, 4-(5-Amino-1-(2,6-difluorobenzoyl)-1H-[1,2,4]triazol-3-ylamino)-benzenesulfonamide, JNJ-7706621, Aurora Kinase Inhibitor I

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実隓匏ヒル衚蚘法:
C15H12F2N6O3S · xC2H3N
CAS番号:
分子量:
394.36
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.54
eCl@ss:
38100201
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 15 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

Fc1c(c(ccc1)F)C(=O)N2NC(=NC2=N)Nc3ccc(cc3)[S](=O)(=O)N

InChI

1S/C15H12F2N6O3S/c16-10-2-1-3-11(17)12(10)13(24)23-14(18)21-15(22-23)20-8-4-6-9(7-5-8)27(19,25)26/h1-7H,(H2,19,25,26)(H3,18,20,21,22)

InChI key

KDKUVYLMPJIGKA-UHFFFAOYSA-N

General description

A cell-permeable triazolylsulfonamido compound that acts a reversible, ATP-competitive kinase inhibitor with selectivities towards Aurora kinases (IC50 = 11 and 15 nM for Aurora-A, Aurora-B, respectively) and Cdk′s (IC50 = 9, 4, and 3 nM for Cdk1/B, Cdk2/A, and Cdk2/E, respectively). Displays antitumor properties both in vitro (IC50 in the range of 112 - 514 nM against various human cancer cell lines) and in a xenograft murine model in vivo (75-100 mg/kg, i.p.).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Aurora Kinase/Cdk
Product competes with ATP.
Reversible: yes
Target IC50: 11 and 15 nM for Aurora-A, Aurora-B, respectively; 9, 4, and 3 nM for Cdk1/B, Cdk2/A, and Cdk2/E, respectively

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Emanuel, S., et al. 2005. Cancer Res.65, 9038.
Lin R., et al. 2005. J. Med. Chem.48, 4208.

Legal Information

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

Disclaimer

Toxicity: Harmful (C)


保管分類

11 - Combustible Solids

WGK

WGK 3

匕火点 (F)

Not applicable

匕火点°C

Not applicable



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