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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.42%
- CAS 番号: 3106831-75-5
- 分子式: C54H54Cl2FN11O6
- 分子量:1042.98
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
Aurora A 120 nM (DC50) |
HSP90 |
体外実験
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. Further protocols information, click here.
体内実験
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%.
化学情報
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CAS 番号 3106831-75-5
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性状 Solid
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分子量 1042.98
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
プロトコル
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
純度とドキュメンテーション
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データシート (281 KB)
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SDS (254 KB)
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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-178472 関連分類
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