Home Cell Cycle Aurora Kinase inhibitor SP-96

research use only

SP-96 Aurora Kinase inhibitor

Cat.No.S9658

SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. This compound can be used for the research of triple negative breast cancer (TNBC).
SP-96 Aurora Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 453.47

Jump to

Quality Control

Batch: S965801 DMSO]91 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.77%
  • Cited in Nature Medicine for its top-tier quality
  • COA
  • NMR
  • HPLC
  • SDS
  • Datasheet
99.77

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (200.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 453.47 Formula

C25H20FN7O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2682114-54-9 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1N=CC(=N1)C2=CC=C3C(=NC=NC3=C2)NC4=CC=CC(=C4)NC(=O)NC5=CC(=CC=C5)F

Mechanism of Action

Targets/IC50/Ki
Aurora B
(Cell-free assay)
0.316 nM
In vitro

SP-96 shows sub-nanomolar potency in Aurora B enzymatic assays (IC50 = 0.316 ± 0.031 nM). This compound shows >2000 fold selectivity against FLT3 and KIT which is important for normal hematopoiesis. Enzyme kinetics of this inhibitor shows non-ATP competitive inhibition which makes it a first-in-class inhibitor. It shows selective growth inhibition in NCI60 screening, including inhibition of MDA-MD-468, a Triple Negative Breast Cancer cell line.
Kinase Assay
Aurora Kinase B enzymatic assay
Kinase inhibition assay is done by measuring kinase activity in a microfluidics assay. The separation of a phosphorylated product from substrate is monitored. The assay is run using a 12-sipper chip on a Caliper EZ Reader II. The recipe used for separation buffer is 100 mM HEPES, 10 mM EDTA, 0.015% Brij-35, 0.1% CR-3. The compound stocks (20 mM in DMSO) are diluted into kinase buffer. 1 μL of desired stock solution is transferred into a 384-well microtiter assay plate. The Aurora B enzyme is diluted in kinase buffer to a concentration of 2 nM. 5 μL of the enzyme mixture is transferred to the assay plate. The inhibitors/Aurora B enzyme are incubated for 60 min with minor shaking. A substrate mix is prepared containing ATP and 5FAM tagged peptide dissolved in kinase buffer described above. 5 μL of the substrate solution is added to the assay plate. Running concentrations are as follows: peptide (1.5 μM), ATP (190 μM), and this compound 12-point ½log dilutions (0.2 mM-0.632 nM). No inhibitor is added for positive control, and no enzymewas added for negative control. For running control, barasertib is used. Percentage inhibition is measured by comparing starting peptide to phosphorylated productpeaks.
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map