| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
Aurora A (IC50 = 12.3 nM)
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|---|---|
| ln Vitro |
AKI603 (0.039-0.6 μM; 48 hours) significantly reduces leukemia cell division[1].
AKI603 (0.039-0.6 μM; 48 hours) has a dose-dependent effect on the phosphorylation of AurA in the NB4, K562, and Jurkat cell lines, but has no effect on the amount of total AurA protein[1]. AKI603 suppresses the growth and colony formation of CML cells resistant to imatinib[1]. AKI603 (0.3-0.6 μM; 48 hours) induces cell cycle arrest with polyploidy accumulation in imatinib-resistant CML cells, inhibiting their ability to proliferate and form colonies[1]. AKI603-induced inhibition of AurA causes leukemia cell senescence in 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]. |
| ln Vivo |
AKI603 (12.5–25 mg/kg; intraperitoneally; every 2 days; for 14 days) prevents xenografted KBM5–T315I cells from growing in nude mice.[1]
AKI603 shows a moderate oral bioavailability (rat 28.7%) and a Cmax of 202.4 μg/L after oral administration (rat 25 mg/kg)[3]. AKI603 has a terminal elimination half-life of 8.9 hours (rat 2.5 mg/kg) after intravenous administration[3]. |
| Cell Assay |
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. |
| Animal Protocol |
Female BALB/c nude mice, with KBM5-T315I cells xenografted[1]
12.5 mg/kg, 25 mg/kg Intraperitoneal injection, every 2 days, for 14 days |
| References |
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| Molecular Formula |
C19H23N9O2
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|---|---|
| Molecular Weight |
409.445021867752
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| Exact Mass |
409.197
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| Elemental Analysis |
C, 55.73; H, 5.66; N, 30.79; O, 7.81
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| CAS # |
1432515-73-5
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| Related CAS # |
1432515-73-5
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| PubChem CID |
72194397
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| Appearance |
White to yellow solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UNKOUVAYOLLXER-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23N9O2/c1-13-11-17(25-24-13)21-16-12-18(27-9-7-26(2)8-10-27)23-19(22-16)20-14-3-5-15(6-4-14)28(29)30/h3-6,11-12H,7-10H2,1-2H3,(H3,20,21,22,23,24,25)
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| Chemical Name |
6-(4-methylpiperazin-1-yl)-4-N-(5-methyl-1H-pyrazol-3-yl)-2-N-(4-nitrophenyl)pyrimidine-2,4-diamine
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| Synonyms |
AKI-603; AKI603; AKI 603
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 82~16.125 mg/mL (200.3~305.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 6.25 mg/mL (15.26 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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