AKI-603 (AKI603)
- CAS No.
- 1432515-73-5
- Chemical Name:
- AKI-603 (AKI603)
- Synonyms
- AKI-603;AKI-603 (AKI603);AKI603, 10 mM in DMSO;AKI603,Aurora Kinase,chronic,CML,leukemia,myeloid,inhibit,imatinib-resistant,Inhibitor;N4-(5-Methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-N2-(4-nitrophenyl)pyrimidine-2,4-diamine;2,4-Pyrimidinediamine, 6-(4-methyl-1-piperazinyl)-N4-(5-methyl-1H-pyrazol-3-yl)-N2-(4-nitrophenyl)-
- CBNumber:
- CB04844451
- Molecular Formula:
- C19H23N9O2
- Molecular Weight:
- 409.45
- MDL Number:
- MFCD28502155
- MOL File:
- 1432515-73-5.mol
- MSDS File:
- SDS
- TDS File:
- TDS
AKI-603 (AKI603) price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 40840 | AKI-603 ≥98% | 1432515-73-5 | 1mg | $116 | 2026-04-30 | Buy |
| Cayman Chemical | 40840 | AKI-603 ≥98% | 1432515-73-5 | 5mg | $521 | 2026-04-30 | Buy |
| Cayman Chemical | 40840 | AKI-603 ≥98% | 1432515-73-5 | 10mg | $924 | 2026-04-30 | Buy |
| Cayman Chemical | 40840 | AKI-603 ≥98% | 1432515-73-5 | 25mg | $2022 | 2026-04-30 | Buy |
| Biosynth | HHC51573 | AKI603 | 1432515-73-5 | 50mg | $1826 | 2026-06-04 | Buy |
AKI-603 (AKI603) Chemical Properties, Uses, Production
Uses
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].
Biological Activity
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]. 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]. 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].
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].
| Animal Model: | Female BALB/c nude mice, with KBM5-T315I cells xenografted[1] |
| Dosage: | 12.5mg/kg, 25mg/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) |
IC 50
Aurora A: 12.3 nM (IC50)
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. [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.
AKI-603 (AKI603) Preparation Products And Raw materials
Raw materials
Preparation Products
AKI-603 (AKI603) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2994 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| Shanghai SuperLan Chemcial Technique Centre | 0-2022843681 15618226720 | chaolaichem@foxmail.com | China | 9996 | 58 |
| BOC Sciences | 16314854226; +8616314854226 | inquiry@bocsci.com | United States | 19852 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6378 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6288 | 58 |
| DC Chemicals | 021-58447131 13564518121 | doncunbiosci@gmail.com | China | 618 | 58 |
| Zhejiang Huida Biotech Co., LTD | 0571-89903022 18679456698 | zilong@hizyme.com | China | 8001 | 58 |
