| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Aurora A-IN-5 (compound 5h) (48 hours) showed potent anti-proliferative activity against a variety of cancer cell lines, with IC50 values of K562 (2.87 μM), MCF-7 (1.50 μM), HeLa (0.85 μM), DU145 (1.85 μM), MOLT-4 (2.25 μM) and MDA-MB-231 (2.04 μM) [1]. Aurora A-IN-5 (0.5 μM, 48 hours) caused abnormal spindle morphology and chromosome disorder in MDA-MB-231 cells [1]. Aurora A-IN-5 (2.5-10 μM, 24 hours) effectively inhibited the division of MDA-MB-231 cells by arresting the cell cycle progress in the G2/M phase [1]. Aurora A-IN-5 (2-20 μM, 24 hours) induced apoptosis in MDA-MB-231 cells in a dose-dependent manner [1]. Aurora A-IN-5 (2 μM, 14 days) effectively inhibited the colony formation of MDA-MB-231 cells, thereby inhibiting their proliferation [1]. Aurora A-IN-5 (0-1 μM) had a potent, selective and dose-dependent inhibitory effect on phosphorylation of Aurora A at Thr288 site. At the same time, Aurora A protein was significantly stabilized in MDA-MB-231 cells by cell thermal displacement analysis (46-62 °C), confirming its direct binding to the target site [1]. Aurora A-IN-5 showed toxicity to mouse embryonic osteoblast MC3T3-E1 cells (IC50 = 7.135 μM), but showed minimal toxicity to normal liver LO2 cells (IC50 = 43.86 μM) [1].
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|---|---|
| ln Vivo |
Aurora A-IN-5 (30 mg/kg, intraperitoneal injection, every two days for 20 days) inhibited tumor growth in a mouse model of MDA-MB-231 xenograft[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MDA-MB-231 cells Tested Concentrations: 2.0 μM Incubation Duration: 14 days Experimental Results: Showed considerably fewer colonies (26 ± 3) compared to the untreated control group (106 ± 3). Apoptosis Analysis[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 2.0 and 20.0 μM Incubation Duration: 24 h Experimental Results: Displayed a concentration-dependent increase in apoptotic cells, ranging from 11.5% at 2.0 μM to 88.6% at 20.0 μM. Cell Cycle Analysis[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 2.5, 5.0 and 10.0 μM Incubation Duration: 24 h Experimental Results: Showed a significant ability to arrest MDA-MB-231 cells in the G2/M phase. The percentage of cells in the G2/M phase gradually increased from 24.2% to 61.8% at 2.5 μM. Immunofluorescence[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 0.5 μM Incubation Duration: 48 h Experimental Results: Displayed abnormal spindle configurations, either monopolar or multipolar, accompanied by various aberrations in chromosome alignment. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice (1-5 weeks) subcutaneously injected with MDA-MB-231 cells[1]
Doses: 30 mg/kg Route of Administration: i.p., every two days for 20 days Experimental Results: Achieved a tumor growth inhibition rate of 73.0%. Exhibited slightly increased body weight without any significant fluctuations throughout the treatment duration. Revealed no significant parenchymal damage or inflammatory cell infiltration in vital organs such as the heart, liver, spleen, lung, and kidney. |
| References |
| Molecular Formula |
C25H29N7O2
|
|---|---|
| Molecular Weight |
459.54
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| Appearance |
Typically exists as solids at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1761 mL | 10.8804 mL | 21.7609 mL | |
| 5 mM | 0.4352 mL | 2.1761 mL | 4.3522 mL | |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1761 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.
Products are for research use only; We do not sell to patients
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