| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AurAP14 (0.1–4 μM) degrades Aurora A, inhibits Aurora A-mediated p53 (Ser315) phosphorylation, and disrupts the non-catalytic protective effect of the proto-oncogene C-MYC in MCF-7 and A549 cells [1]. AurAP14 (0.5 μM, 24 h) inhibits the migration and colony formation of A549 cells and arrests A549 cells in the S and G2/M phases [1]. AurAP14 (0.5 μM, 24–48 h) induces apoptosis in A549 cells [1].
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|---|---|
| ln Vivo |
AurAP14 (30 mg/kg, intraperitoneal injection, every 2 days for 21 days) achieved tumor growth inhibition in A549 and A549/PTR mouse nude transplantation models [1].
|
| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: A549 cells Tested Concentrations: 0.5 μM Incubation Duration: 24 h Experimental Results: Arrested A549 cells in the S and G2/M phases. Apoptosis Analysis[1] Cell Types: A549 cells Tested Concentrations: 0.5 μM Incubation Duration: 12, 24, 48 h Experimental Results: Induced apoptosis in A549 cells. |
| Animal Protocol |
Animal/Disease Models: A549 cells and A549/PTR cells (1.5×107 cells/100 μL) were subcutaneously implanted into the armpits of 5-week-old male BALB/c nude mice[1]
Doses: 30 mg/kg Route of Administration: i.p., once every 2 days, 21 days Experimental Results: Achieved tumor growth inhibition (TGI) rates of 59.6% and 56.6% in A549 and A549/PTR nude mouse xenograft models, respectively. Showed no significant changes in body weight and no obvious organ toxicity. Reduced Aurora A expression in tumor tissues by more than 50%. |
| References |
| Molecular Formula |
C54H54CL2FN11O6
|
|---|---|
| Molecular Weight |
1042.98
|
| Appearance |
Light yellow to yellow solid
|
| SMILES |
COC1=CC(NC2=NC3=C(CN=C(C4=C3C=CC(Cl)=C4)C5=C(C=CC=C5F)OC)C=N2)=CC=C1C(NCCOCCNC(CCCCCC#CC6=CN(C7=C6C(Cl)=NC(N)=N7)CC8=NC=C(C(OC)=C8C)C)=O)=O
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~95.9 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (2.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9588 mL | 4.7940 mL | 9.5879 mL | |
| 5 mM | 0.1918 mL | 0.9588 mL | 1.9176 mL | |
| 10 mM | 0.0959 mL | 0.4794 mL | 0.9588 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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