Aurora A Inhibitor I (TC-S 7010) - Moligand™, 10mM in DMSO , Inhibitor of aurora kinase A;Inhibitor of aurora kinase B, CAS No.1158838-45-9, Inhibitor of aurora kinase A;Inhibitor of aurora kinase B

CAS: 1158838-45-9 Cat. No.: A408991 Molecular Weight: 588.07 EC Number: 806-027-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Aurora A Inhibitor I (TC-S 7010) is a novel, potent, and selective inhibitor ofAurora AwithIC50of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggersapoptosisthrough the ROS-med
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. 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. 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.

In vivo

Cell Data

cell lines：Human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs)

Concentrations：0.1 nM - 10 μM, dissolved in medium lacking serum and glutamine (dissolved in DMSO as stock solution)

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Synonyms

N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Aurora A Inhibitor I (TC-S 7010) 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. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the R

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of aurora kinase A;Inhibitor of aurora kinase B

Names and Identifiers

• Isomeric 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
• WGK Germany: 3
• Molecular Weight: 588.07
• Reaxy-Rn: 19963522
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19963522&ln=

Associated Targets(Human)

AURKA Tchem Aurora kinase A (3 Activities)

Discover Target: AURKA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B (1 Activities)

Discover Target: AURKB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 62 mg/mL (198.43 mM); Ethanol: 62 mg/mL (198.43 mM); Water: Insoluble