Home Tools

TCS7010

Catalog No. T6767 CAS 1158838-45-9

Synonyms: Aurora A Inhibitor I

TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

TCS7010, CAS 1158838-45-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 127.00
25 mg	In stock	$ 230.00
50 mg	In stock	$ 398.00
100 mg	In stock	$ 592.00
500 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 94.00

Bulk Inquiry

Select Batch

Purity: 99.69%

Purity: 98.49%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.
Targets&IC50	Aurora A:3.4 nM
In vitro	Aurora A Inhibitor I is a 2,4-dianilinopyrimidine that selectively and potently inhibits Aurora A. Aurora A Inhibitor I effectively inhibits the proliferation of HCT116 and HT29 cells, with IC50 of 190 nM and 2.9 μM, respectively. The Aurora A selectivity of Aurora A Inhibitor I against Aurora B depends on a single amino acid (Thr217) of Aurora A. [1] In KCL-22 cells, Aurora A Inhibitor I (1-5 μM) increases G2/M cell fraction, induces histone H3 serine 10 phosphorylation, and suppresses mitotic Aurora A autophosphorylation on Thr288. Aurora A Inhibitor I (0.5-5 μM) also suppresses cell proliferation in KCL-22 cells, as well as BCR-ABL-negative leukemia cell lines KG-1 and HL-60. Aurora A Inhibitor I effectively induces apoptosis in KCL-22 cells at 5 μM. [2] In a recent study, Aurora A Inhibitor I is also found to inhibit cell growth of HCT116, HT29, and HeLa cells, with IC50 of 377.6 nM, 5.6 μM, and 416 nM. [3]
Kinase Assay	Auroras A and B Inhibition Assays: Both Auroras A and B are assayed in ELISA format using a GST fusion (pGEX-4T) of the N-terminus of Histone H3 (aa 1?18) as substrate. Plates are coated with 2 μg/mL substrate in PBS then blocked with 1 mg/mL I-block in PBS. Kinase reactions are run for 40 min with 5 ng/mL (0.16 nM) Aurora A or 45 ng/mL (1.1 nM) Aurora B at 30 μM ATP (~ Km) in kinase buffer. Final DMSO concentration is 4%. Product is detected by incubation with antiphosphohistone H3 (Ser10) 6 g3 mouse monoclonal antibody and sheep-anti-mouse HRP conjugate, followed by washing and addition of TMB substrate. After quenching with 1 M phosphoric acid, plates are read at 450 nM.
Cell Research	Cells are seeded in 384-well plates on day 0 in 50 μL of complete medium and incubated overnight in a 5% CO2 atmosphere at 37 °C. On day 1, 10 μL of Aurora A Inhibitor I is added. On day 4, plates are allowed to reach room temperature, and 30 μL Cell Titer-Glo reagent is added to each well to measure total ATP levels. Plates are read after shaking 15 min at room temperature.(Only for Reference)

Synonyms	Aurora A Inhibitor I
Molecular Weight	588.07
Formula	C31H31ClFN7O2
CAS No.	1158838-45-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 58.8 mg/mL (100 mM)

References and Literature

1. Aliagas-Martin I, et al. J Med Chem, 2009, 52(10), 3300-3307. 2. Yuan H, et al. Carcinogenesis, 2012, 33(2), 285-293. 3. Kwiatkowski N, et al. ACS Chem Biol, 2012, 7(1), 185-196. 4. Rawson TE, et al. J Med Chem, 2008, 51(15), 4465-4475.

Citations

1. Chen H, Hu J, Xiong X, et al.AURKA inhibition induces Ewing’s sarcoma apoptosis and ferroptosis through NPM1/YAP1 axis.Cell Death & Disease.2024, 15(1): 99.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Bioactive Compound Library Epigenetics Compound Library Cell Cycle Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Apoptosis Compound Library Kinase Inhibitor Library

Related Products

Related compounds with same targets

Diosgenin glucoside CSRM617 hydrochloride EC359 10-Gingerol Rimiducid CK2/ERK8-IN-1 Schisandrin C Xanthatin

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TCS7010 1158838-45-9 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase TCS 7010 inhibit Aurora A Inhibitor I Inhibitor TCS-7010 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.