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AKI603

Catalog No. T64338 CAS 1432515-73-5

Synonyms: 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].

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AKI603, CAS 1432515-73-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 116.00
5 mg	In stock	$ 287.00
10 mg	In stock	$ 478.00
25 mg	In stock	$ 789.00
50 mg	In stock	$ 1,080.00
100 mg	In stock	$ 1,480.00
500 mg	In stock	$ 2,970.00
1 mL * 10 mM (in DMSO)	In stock	$ 318.00

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Purity: 99.81%

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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
Molecular Weight	409.45
Formula	C19H23N9O2
CAS No.	1432515-73-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (293.07 mM), Sonication is recommended.

References and Literature

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. 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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Cell Cycle Compound Library Bioactive Compounds Library Max Epigenetics Compound Library Bioactive Compound Library Anti-Cancer Compound Library Kinase Inhibitor Library NO PAINS Compound Library

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Keywords

AKI603 1432515-73-5 Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase chronic CML leukemia myeloid inhibit imatinib-resistant Inhibitor AKI 603 AKI-603 inhibitor

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