2. PROTAC Epigenetics Cell Cycle/DNA Damage Neuronal Signaling Cytoskeleton Protein Tyrosine Kinase/RTK
  3. PROTACs Aurora Kinase AAK1 Cyclin G-associated Kinase (GAK) Mps1 FAK
  4. dAurAB5

dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).

For research use only. We do not sell to patients.

dAurAB5

dAurAB5 Chemical Structure

CAS No. : 3115765-45-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

dAurAB5 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236)[1].

IC50 & Target[1]

Cereblon

 

Aurora-A

8.8 nM (DC50)

Aurora-B

6.1 nM (DC50)

In Vitro

dAurAB5 (500 nM, 24 h) induces significant degradation of Aurora-A and Aurora-B, with degradation rates of 84% and 82%[1].
dAurAB5 (500 nM, 24 h) reduces N-Myc levels by 45% in IMR32 cells[1].
dAurAB5 (100 nM, 4 h) degrades 83% of Aurora-A and 95% of Aurora-B in IMR32 cells[1].
dAurAB5 (200 nM, 6 h) decreases the abundance Aurora-A and the levels of AAK1, PTK2, GAK, TTK, but does not downregulated Aurora-B abundance in the MYCN-amplified Kelly neuroblastoma cells[1].
dAurAB5 (0-1000 nM, 24 h) reduces cell viability in IMR32 cells, but has minimal cytotoxicity in HEK293 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

dAurAB5 Related Antibodies

Western Blot Analysis[1]

Cell Line: IMR32 cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Reduced N-Myc levels by 45%.

Western Blot Analysis[1]

Cell Line: IMR32 cells
Concentration: 100 nM
Incubation Time: 4 h
Result: Degraded 83% of Aurora-A and 95% of Aurora-B.

Cell Viability Assay[1]

Cell Line: IMR32 cells
Concentration: 0, 10, 100, 1000 nM
Incubation Time: 24 h
Result: Significant reduced cell viability, with 45% reduction in cell viability at 100 nM and 55% reduction in cell viability at 1 μM.
Molecular Weight

819.91

Formula

C42H49N11O7
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(NCCCCCC(N1CCN(C2=CC=C(NC3=NC(NC4CCCCC4)=C5N=CNC5=N3)C=C2)CC1)=O)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (121.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2196 mL 6.0982 mL 12.1965 mL
5 mM 0.2439 mL 1.2196 mL 2.4393 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (6.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
DMSO 1 mM 1.2196 mL 6.0982 mL 12.1965 mL 30.4912 mL
5 mM 0.2439 mL 1.2196 mL 2.4393 mL 6.0982 mL
10 mM 0.1220 mL 0.6098 mL 1.2196 mL 3.0491 mL
15 mM 0.0813 mL 0.4065 mL 0.8131 mL 2.0327 mL
20 mM 0.0610 mL 0.3049 mL 0.6098 mL 1.5246 mL
25 mM 0.0488 mL 0.2439 mL 0.4879 mL 1.2196 mL
30 mM 0.0407 mL 0.2033 mL 0.4065 mL 1.0164 mL
40 mM 0.0305 mL 0.1525 mL 0.3049 mL 0.7623 mL
50 mM 0.0244 mL 0.1220 mL 0.2439 mL 0.6098 mL
60 mM 0.0203 mL 0.1016 mL 0.2033 mL 0.5082 mL
80 mM 0.0152 mL 0.0762 mL 0.1525 mL 0.3811 mL
100 mM 0.0122 mL 0.0610 mL 0.1220 mL 0.3049 mL
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dAurAB5 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dAurAB53115765-45-9dAurAB 5dAurAB-5PROTACsAurora KinaseAAK1Cyclin G-associated Kinase (GAK)Mps1FAKAdaptor-associated Kinase 1AP2-associated kinase 1Auxilin 2Monopolar spindle 1PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasePROTACIMR32 neuroblastoma cellsneuroblastomadegraderInhibitorinhibitorinhibit

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