1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. AKI603

AKI603 

Cat. No.: HY-123159 Purity: 98.05%
Handling Instructions

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

AKI603 Chemical Structure

CAS No. : 1432515-73-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 385 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 5800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 11000 In-stock
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50 mg USD 17000 In-stock
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100 mg USD 25000 In-stock
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Description

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[1][2].

IC50 & Target[1]

Aurora A

12.3 nM (IC50)

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].

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 Cmax (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].

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%), Cmax (202.4 μg/L), T1/2 (8.9 h)
Molecular Weight

409.45

Formula

C₁₉H₂₃N₉O₂

CAS No.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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AKI603
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HY-123159
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