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Art. -Nr.: HY-137344

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dAURK-4

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dAURK-4 is a selective AURKA PROTAC degrader. dAURK-4 promotes ubiquitination and degradation of AURKA. dAURK-4 can be used in the research of glioblastoma and multiple myeloma.
(Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W004640)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.93%
CAS. Nr.: 2705844-81-9
Formel: C₅₂H₅₂ClFN₈O₁₂
Molecular Weight:1035.47

Speicherung:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

dAURK-4 Chemical Structure

CAS. Nr.: 2705844-81-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

dAURK-4 is a selective AURKA PROTAC degrader. dAURK-4 promotes ubiquitination and degradation of AURKA. dAURK-4 can be used in the research of glioblastoma and multiple myeloma^[1]^[2]. (Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W004640)).

IC₅₀ & Target^[2]

Aurora A

Cereblon

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

dAURK-4 (1 μM; 5 h) potently and selectively degrades AURKA in MOLT-4 T-lymphoblastic leukemia cells, while exhibits weak activity against AURKB^[2].
dAURK-4 (125-1000 nM; 4-24 h) induces dose-dependent degradation of AURKA in MM.1S multiple myeloma cells, and achieves nearly complete degradation at concentrations ≥250 nM^[2].
dAURK-4 (0.0001-100 μM; 72 h) exhibits better antiproliferative activity than Alisertib (HY-10971) in MM.1S multiple myeloma cells, with stronger potency at low concentrations and more significant inhibitory effects on cell viability at high concentrations^[2].

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

Western Blot Analysis^[2]

Cell Line:

MM.1S multiple myeloma cells
Concentration:

125-1000 nM (4 h incubation); 125-1000 nM (24 h incubation)
Incubation Time:

4 h; 24 h
Result:

Induced dose-dependent degradation of AURKA at both 4 h and 24 h.
Caused near-complete loss of AURKA protein at concentrations of 250 nM and higher for both incubation times.

Cell Viability Assay^[2]

Cell Line:

human MM.1S multiple myeloma cells
Concentration:

0.0001-100 μM
Incubation Time:

72 h
Result:

Reduced relative cell viability to ≤0.6 at concentrations of 0.1 μM and above.
Reduced relative viability to ~0.2 at 10 μM.
Exhibited superior antiproliferative activity compared to parental inhibitor alisertib, which only achieved comparable viability reduction at 1 μM and above and reduced viability to ~0.0 at 10 μM.

Chemical Information

CAS. Nr. 2705844-81-9
Appearance Solid
Molecular Weight 1035.47
Formel C₅₂H₅₂ClFN₈O₁₂
Color Off-white to light yellow
SMILES

O=C(N(C1C(NC(CC1)=O)=O)C2=O)C3=C2C=CC=C3OCC(NCCCOCCOCCOCCCNC(C4=CC=C(NC5=NC=C6C(C(C=CC(Cl)=C7)=C7C(C8=C(F)C=CC=C8OC)=NC6)=N5)C=C4OC)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (96.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9657 mL

4.8287 mL

9.6574 mL

5 mM

0.1931 mL

0.9657 mL

1.9315 mL

10 mM

0.0966 mL

0.4829 mL

0.9657 mL

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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Leconte G A. Developing a Generalizable Approach to Improve the Blood Brain Barrier Permeability of Proteolysis Targeting Chimeras Through Prodrugs[D]. University of California, San Diego, 2023.

[2]. Donovan KA, et al. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. 2020 Dec 10;183(6):1714-1731.e10. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.9657 mL	4.8287 mL	9.6575 mL	24.1436 mL
	5 mM	0.1931 mL	0.9657 mL	1.9315 mL	4.8287 mL
	10 mM	0.0966 mL	0.4829 mL	0.9657 mL	2.4144 mL
	15 mM	0.0644 mL	0.3219 mL	0.6438 mL	1.6096 mL
	20 mM	0.0483 mL	0.2414 mL	0.4829 mL	1.2072 mL
	25 mM	0.0386 mL	0.1931 mL	0.3863 mL	0.9657 mL
	30 mM	0.0322 mL	0.1610 mL	0.3219 mL	0.8048 mL
	40 mM	0.0241 mL	0.1207 mL	0.2414 mL	0.6036 mL
	50 mM	0.0193 mL	0.0966 mL	0.1931 mL	0.4829 mL
	60 mM	0.0161 mL	0.0805 mL	0.1610 mL	0.4024 mL
	80 mM	0.0121 mL	0.0604 mL	0.1207 mL	0.3018 mL

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
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dAURK-4

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Heterocyclic Compound Library

PROTAC Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dAURK-4

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Heterocyclic Compound Library

PROTAC Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dAURK-4 Related Classifications

HY-137344 Related Classifications