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Cat. No.: HY-178343

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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.

Formula: C₂₅H₂₉N₇O₂
Molecular Weight:459.54

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

Aurora A-IN-5 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Aurora A

0.02 μM (IC₅₀)

All Aurora Kinase Isoforms :

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.

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	C_max	AUC_0-∞	V_d	T_1/2	CL	MRT_0-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.

Chemical Information

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Long L, et al. Discovery of a Potent and Highly Selective Inhibitor of Aurora A Kinase. ACS Med Chem Lett. 2025 Sep 17;16(10):2057-2069. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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