AKI603

Name: AKI603
Brand: MedChemExpress
SKU: HY-123159
Rating: 4.5 (1 reviews)

Cat. No.: HY-123159 Purity: 98.03%: FAQs
Data Sheet SDS COA Handling Instructions

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AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC₅₀ of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.

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

AKI603 Chemical Structure

CAS No. : 1432515-73-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 330	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 330	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 810	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1215	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1701	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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View All Isoforms

Aurora Kinase Aurora A Aurora B Aurora C

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Aurora A

12.3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.15 μM Compound: 7u	Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
A549	IC₅₀	0.723 μM Compound: 7u	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
DU-145	IC₅₀	1.2 μM Compound: 7u	Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
HCT-116	IC₅₀	1.63 μM Compound: 7u	Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
HeLa	IC₅₀	0.331 μM Compound: 7u	Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
HL-60	IC₅₀	0.0698 μM Compound: 7u	Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
K562	IC₅₀	0.137 μM Compound: 7u	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
MCF7	IC₅₀	0.424 μM Compound: 7u	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
MDA-MB-231	IC₅₀	0.0844 μM Compound: 7u	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
MOLT-4	IC₅₀	0.0181 μM Compound: 7u	Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
NCI-N87	IC₅₀	3.88 μM Compound: 7u	Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
PANC-1	IC₅₀	0.442 μM Compound: 7u	Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
PC-3	IC₅₀	1.09 μM Compound: 7u	Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
SK-BR-3	IC₅₀	0.437 μM Compound: 7u	Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
U-937	IC₅₀	0.0433 μM Compound: 7u	Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]

In Vitro

AKI603 (0.039-0.6 μM; 48 hours) extensively inhibits proliferation of leukemia cells^[1].
AKI603 (0.039-0.6 μM; 48 hours) significantly inhibits the phosphorylation of AurA in NB4, K562, and Jurkat cell lines in a dose-dependent manner while the level of total AurA protein is not changed^[1].
AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells^[1].
AKI603 (0.3-0.6 μM; 48 hours) inhibits cell proliferation and colony formation capacities in imatinib-resistant CML cells by inducing cell cycle arrest with polyploidy accumulation^[1].
Inhibition of AurA by AKI603 induces leukemia cell senescence in both BCR-ABL wild type and T315I mutation cells^[1].
AKI603 exhibits inhibitory activities on breast cancer cell proliferation, such as SUM149 (IC₅₀=2.04), BT549 (IC₅₀=0.86), MCF-7 (IC₅₀=0.97), MCF-7-Epi (IC₅₀=21.01), Sk-br-3 (IC₅₀=0.73), MDA-MB-231 (IC₅₀=3.49), MDA-MB-453 (MTT, IC₅₀=0.18; Cell counting, IC₅₀=0.19), MDA-MB-468 (MTT, IC₅₀=0.15; Cell counting, IC₅₀=0.17)^[2].

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

Cell Proliferation Assay^[1]

Cell Line:	U937 cells, HL-60 cells, NB4 cells, KBM5 cells, K562 cells, Jurkat cells
Concentration:	0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM
Incubation Time:	48 hours
Result:	Inhibited all the tested cell lines.

Western Blot Analysis^[1]

Cell Line:	NB4 cells, K562 cells, Jurkat cells
Concentration:	0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM
Incubation Time:	48 hours
Result:	Inhibited the phosphorylation of AurA Thr288 (p-AurA).

Cell Cycle Analysis^[1]

Cell Line:	K562, K562/G, 32D-p210 and 32D-T315I cells
Concentration:	0.3 μM, 0.6 μM
Incubation Time:	48 hours
Result:	Induced polyploidization in the tested cells.

In Vivo

AKI603 (12.5-25 mg/kg; i.p.; every 2 days; for 14 days) abrogates the growth of xenografted KBM5-T315I cells in nude mice^[1].
AKI603 exhibits moderate oral bioavailability (rat 28.7%) and C_max (rat 202.4 μg/L) following oral administration (rat 25 mg/kg)^[3].
AKI603 exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg)^[3].

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

Animal Model:	Female BALB/c nude mice, with KBM5-T315I cells xenografted^[1]
Dosage:	12.5 mg/kg, 25 mg/kg
Administration:	Intraperitoneal injection, every 2 days, for 14 days
Result:	Significantly inhibited the growth of tumors.

Animal Model:	SD rats (220-280 g)^[3]
Dosage:	2.5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:	Intravenous injection, oral administration
Result:	Oral bioavailability (28.7%), C_max (202.4 μg/L), T_1/2 (8.9 h)

Molecular Weight

409.45

Formula

C₁₉H₂₃N₉O₂

CAS No.

1432515-73-5

Appearance

Solid

Color

White to yellow

SMILES

O=[N+]([O-])C1=CC=C(C=C1)NC2=NC(N3CCN(CC3)C)=CC(NC4=NNC(C)=C4)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (305.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4423 mL	12.2115 mL	24.4230 mL
5 mM	0.4885 mL	2.4423 mL	4.8846 mL
10 mM	0.2442 mL	1.2212 mL	2.4423 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 6.25 mg/mL (15.26 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 6.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.03%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (249 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Le-Xun Wang, et al. Aurora A Kinase Inhibitor AKI603 Induces Cellular Senescence in Chronic Myeloid Leukemia Cells Harboring T315I Mutation. Sci Rep. 2016 Nov 8;6:35533. [Content Brief]

[2]. Fei-Meng Zheng, et al. A novel small molecule aurora kinase inhibitor attenuates breast tumor-initiating cells and overcomes drug resistance. Mol Cancer Ther. 2014 Aug;13(8):1991-2003. [Content Brief]

[3]. Zhenzhen Zhao, et al. Determination of a novel Aurora-A (AurA) kinase AKI603 by UPLC-MS/MS and its application to a bioavailability study in rat. J Pharm Biomed Anal. 2016 Jun 5;125:303-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4423 mL	12.2115 mL	24.4230 mL	61.0575 mL
	5 mM	0.4885 mL	2.4423 mL	4.8846 mL	12.2115 mL
	10 mM	0.2442 mL	1.2212 mL	2.4423 mL	6.1058 mL
	15 mM	0.1628 mL	0.8141 mL	1.6282 mL	4.0705 mL
	20 mM	0.1221 mL	0.6106 mL	1.2212 mL	3.0529 mL
	25 mM	0.0977 mL	0.4885 mL	0.9769 mL	2.4423 mL
	30 mM	0.0814 mL	0.4071 mL	0.8141 mL	2.0353 mL
	40 mM	0.0611 mL	0.3053 mL	0.6106 mL	1.5264 mL
	50 mM	0.0488 mL	0.2442 mL	0.4885 mL	1.2212 mL
	60 mM	0.0407 mL	0.2035 mL	0.4071 mL	1.0176 mL
	80 mM	0.0305 mL	0.1526 mL	0.3053 mL	0.7632 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6106 mL

AKI603 Related Classifications

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:

AKI6031432515-73-5AKI 603AKI-603Aurora Kinasechronicmyeloidleukemiaimatinib-resistantCMLInhibitorinhibitorinhibit

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AKI603

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