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AKI603

Name: AKI603
Brand: TargetMol
SKU: T64338
Price: 60 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T64338Cas No. 1432515-73-5

Alias AKI-603, AKI 603

AKI603 is a novel small molecule inhibitor of Aurora kinase A (AurA)(IC50 = 12.3 nM). AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].

AKI603

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Purity: 99.78%

Catalog No. T64338Alias AKI-603, AKI 603Cas No. 1432515-73-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$60	In Stock	In Stock
5 mg	$148	In Stock	In Stock
10 mg	$223	In Stock	In Stock
25 mg	$401	In Stock	In Stock
50 mg	$591	In Stock	In Stock
100 mg	$833	In Stock	In Stock
200 mg	$1,120	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$163	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.78%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	AKI603 is a novel small molecule inhibitor of Aurora kinase A (AurA)(IC50 = 12.3 nM). AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].
Targets&IC50	Aurora A:12.3 nM
In vitro	AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells[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 as well as 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].
In vivo	AKI603 exhibits moderate oral bioavailability and Cmax following oral administration[3]. AKI603 exhibits terminal elimination half-life following intravenous administration[3]. AKI603 abrogates the growth of xenografted KBM5-T315I cells in nude mice[1].
Cell Research	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]. 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].
Animal Research	AKI603 (12.5-25?mg/kg; i.p.; every 2 days; for 14 days; female BALB/c nude mice with KBM5-T315I cells xenografted) abrogates the growth of tumors[1]. Pharmacokinetic Analysis shows that AKI603 exhibits moderate oral bioavailability (rat 28.7%) and Cmax (rat 202.4 μg/L) following oral administration (rat 25 mg/kg)[3]. AKI603 also exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg)[3].
Synonyms	AKI-603, AKI 603

Chemical Properties

Molecular Weight	409.45
Formula	C₁₉H₂₃N₉O₂
Cas No.	1432515-73-5
Smiles	CN1CCN(CC1)c1cc(Nc2cc(C)[nH]n2)nc(Nc2ccc(cc2)[N+]([O-])=O)n1
Relative Density.	1.407 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 120 mg/mL (293.08 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4423 mL	12.2115 mL	24.4230 mL	122.1150 mL
5 mM	0.4885 mL	2.4423 mL	4.8846 mL	24.4230 mL
10 mM	0.2442 mL	1.2212 mL	2.4423 mL	12.2115 mL
20 mM	0.1221 mL	0.6106 mL	1.2212 mL	6.1058 mL
50 mM	0.0488 mL	0.2442 mL	0.4885 mL	2.4423 mL
100 mM	0.0244 mL	0.1221 mL	0.2442 mL	1.2212 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc