2. Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. Aurora Kinase Apoptosis
  4. Aurora A-IN-5

Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research.

For research use only. We do not sell to patients.

Aurora A-IN-5

Aurora A-IN-5 Chemical Structure

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Aurora A-IN-5 Related Antibodies

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Description

Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research[1].

IC50 & Target[1]

Aurora A

0.02 μM (IC50)

In Vitro

Aurora A-IN-5 (compound 5h) (48 h) shows strong antiproliferative activity against a panel of cancer cell lines, with IC50 values of 2.87 μM (K562), 1.50 μM (MCF-7), 0.85 μM (HeLa), 1.85 μM (DU145), 2.25 μM (MOLT-4), and 2.04μM (MDA-MB-231)[1].
Aurora A-IN-5 (0.5 μM, 48 h) causes abnormalities in spindle morphology and chromosomal organization in MDA-MB-231 cells[1].
Aurora A-IN-5 (2.5-10 μM, 24 h) effectively inhibits MDA-MB-231 cell division by halting cell cycle progression at the G2/M phase[1].
Aurora A-IN-5 (2-20 μM, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner[1].
Aurora A-IN-5 (2 μM, 14 days) effectively suppresses colony formation in MDA-MB-231 cells, thus inhibiting their proliferation[1].
Aurora A-IN-5 (0-1 μM) exhibits potent, selective, and dose-dependent inhibition of Aurora A phosphorylation at Thr288, with concurrent demonstration of target engagement in MDA-MB-231 cells through significant stabilization of Aurora A protein in a cellular thermal shift assay (46-62 °C)[1].
Aurora A-IN-5 exhibits toxicity in mouse embryonic osteoblast MC3T3-E1 cells (IC50 = 7.135 μM) but exhibits minimal toxicity toward normal liver LO2 cells (IC50 = 43.86 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Aurora A-IN-5 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.0 μM
Incubation Time: 14 days
Result: Showed considerably fewer colonies (26 ± 3) compared to the untreated control group (106 ± 3).

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.0 and 20.0 μM
Incubation Time: 24 h
Result: Displayed a concentration-dependent increase in apoptotic cells, ranging from 11.5% at 2.0 μM to 88.6% at 20.0 μM.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5, 5.0 and 10.0 μM
Incubation Time: 24 h
Result: Showed a significant ability to arrest MDA-MB-231 cells in the G2/M phase.
The percentage of cells in the G2/M phase gradually increased from 24.2% to 61.8% at 2.5 μM.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM
Incubation Time: 48 h
Result: Displayed abnormal spindle configurations, either monopolar or multipolar, accompanied by various aberrations in chromosome alignment.
Parmacokinetics
Species Dose Route Note Cmax AUC0-∞ Vd T1/2 CL MRT0-t F
Rat[1] 10 mg/kg p.o. SD Rats 14.95 ng/mL 88.83 ng·h/mL 216.80 L/kg 5.08 h 27.51 L/h/kg 7.55 h 7.7 %
Rat[1] 5 mg/kg i.v. SD Rats 414.28 ng/mL 578.22 ng·h/mL 12.06 L/kg 3.85 h 2.08 L/h/kg 2.93 h /
In Vivo

Aurora A-IN-5 (30 mg/kg, i.p., every two days for 20 days) inhibits tumor growth in MDA-MB-231 xenograft mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice (1-5 weeks) subcutaneously injected with MDA-MB-231 cells[1]
Dosage: 30 mg/kg
Administration: i.p., every two days for 20 days
Result: Achieved a tumor growth inhibition rate of 73.0%.
Exhibited slightly increased body weight without any significant fluctuations throughout the treatment duration.
Revealed no significant parenchymal damage or inflammatory cell infiltration in vital organs such as the heart, liver, spleen, lung, and kidney.
Molecular Weight

459.54

Formula

C25H29N7O2
SMILES

CN1CCN(C2=CC3=NC(C4=CC=CC(OC)=C4OC)=NC(NC5=NNC(C)=C5)=C3C=C2)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Aurora A-IN-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Aurora A-IN-5Aurora KinaseApoptosisAurora AautophosphorylationMDA-MB-231xenograft modelsbreastcervicalprostatelymphomaK562HelaMCF-7DU145MOLT-4Inhibitorinhibitorinhibit

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