AurAP14
Based on 1 Customer Validation
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 can form a stable ternary complex with Aurora A kinase and HSP90, recruiting cullin family E3 ubiquitin ligases and MDM2 to mediate the ubiquitination and proteasome degradation of Aurora A kinase. AurAP14 increases p53 levels and decreases C-MYC levels; AurAP14 induces Apoptosis. AurAP14 can be used in the study of non-small cell lung cancer.
(Pink: Aurora A ligand (HY-10971); Blue: HSP90 ligand (HY-W437598); Black: linker).
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- Pureté: 99.42%
- CAS No.: 3106831-75-5
- Formule: C54H54Cl2FN11O6
- Masse moléculaire:1042.98
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Aurora A 120 nM (DC50) |
HSP90 |
In Vitro
AurAP14 (0.1-4 μM) degrades Aurora A, inhibits Aurora A-mediated phosphorylation of p53 (Ser315), and disrupts the non-catalytic protection of the proto-oncoprotein C-MYC in MCF-7and A549 cells[1].
AurAP14 (0.5 μM, 24 h) inhibits A549 cells migration and colony formation 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model: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]
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Dosage:30 mg/kg
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Administration:i.p., once every 2 days, 21 days
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Result: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%.
Chemical Information
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CAS No. 3106831-75-5
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Appearance Solid
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Masse moléculaire 1042.98
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Formule C54H54Cl2FN11O6
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Color Light yellow to yellow
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (95.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.40 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9588 mL | 4.7940 mL | 9.5879 mL | 23.9698 mL |
| 5 mM | 0.1918 mL | 0.9588 mL | 1.9176 mL | 4.7940 mL | |
| 10 mM | 0.0959 mL | 0.4794 mL | 0.9588 mL | 2.3970 mL | |
| 15 mM | 0.0639 mL | 0.3196 mL | 0.6392 mL | 1.5980 mL | |
| 20 mM | 0.0479 mL | 0.2397 mL | 0.4794 mL | 1.1985 mL | |
| 25 mM | 0.0384 mL | 0.1918 mL | 0.3835 mL | 0.9588 mL | |
| 30 mM | 0.0320 mL | 0.1598 mL | 0.3196 mL | 0.7990 mL | |
| 40 mM | 0.0240 mL | 0.1198 mL | 0.2397 mL | 0.5992 mL | |
| 50 mM | 0.0192 mL | 0.0959 mL | 0.1918 mL | 0.4794 mL | |
| 60 mM | 0.0160 mL | 0.0799 mL | 0.1598 mL | 0.3995 mL | |
| 80 mM | 0.0120 mL | 0.0599 mL | 0.1198 mL | 0.2996 mL |
AurAP14 Related Classifications
HY-178472 Related Classifications
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