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TCS7010 (Aurora A Inhibitor I) Aurora Kinase inhibitor

Name: TCS7010 (Aurora A Inhibitor I)
Brand: Selleck Chemicals
SKU: S1451
Rating: 5 (37 reviews)

Cat.No.S1451

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, and triggers apoptosis through the ROS-mediated UPR signalling pathway.

Chemical Structure

Molecular Weight: 588.07

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Quality Control

Batch: Purity: 99.64%

99.64

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Casein Kinase
Other Aurora Kinase Inhibitors	Hesperadin Barasertib-HQPA (AZD2811) Alisertib (MLN8237) Tozasertib (VX-680) ZM 447439 MLN8054 Danusertib (PHA-739358) MK-5108 AMG-900 PHA-680632

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
HCT116 cells	Proliferation assay	4 days	Antiproliferative activity against human HCT116 cells after 4 days by celltiter assay, IC50=0.19 μM
HT-29 cells	Proliferation assay	4 days	Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay, IC50=2.9 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	588.07	Formula	C₃₁H₃₁ClFN₇O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1158838-45-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	TC-S 7010			Smiles	CCN1CCN(CC1)C(=O)CC2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=C(C=C4)C(=O)NC5=CC=CC=C5Cl)F

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (42.51 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.13mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Features	Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A.
Targets/IC₅₀/Ki	Aurora A (Cell-free assay) 3.4 nM
In vitro	TCS7010 (Aurora A Inhibitor I) is a 2,4-dianilinopyrimidine that selectively and potently inhibits Aurora A. It effectively inhibits the proliferation of HCT116 and HT29 cells, with IC50 of 190 nM and 2.9 μM, respectively. The Aurora A selectivity of this compound against Aurora B depends on a single amino acid (Thr217) of Aurora A. In KCL-22 cells, it (1-5 μM) increases G2/M cell fraction, induces histone H3 serine 10 phosphorylation, and suppresses mitotic Aurora A autophosphorylation on Thr288. It (0.5-5 μM) also suppresses cell proliferation in KCL-22 cells, as well as BCR-ABL-negative leukaemia cell lines KG-1 and HL-60. This compound effectively induces apoptosis in KCL-22 cells at 5 μM. In a recent study, it 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.
Kinase Assay	Aurora A and B Inhibition Assays
Kinase Assay	TCS7010 (Aurora A Inhibitor I) is assayed in ELISA format using a GST fusion (pGEX-4T) of the N-terminus of Histone H3 (aa 1−18) as substrate for both Auroras A and B. 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 (~ K_m) in kinase buffer. Final DMSO concentration is 4%. Product is detected by incubation with antiphosphohistone H3 (Ser10) 6G3 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19402633/ [2] https://pubmed.ncbi.nlm.nih.gov/22116466/ [3] https://pubmed.ncbi.nlm.nih.gov/21992004/ [4] https://pubmed.ncbi.nlm.nih.gov/18630890/ [5] https://www.nature.com/articles/s41467-018-05694-4

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