| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C52H52ClFN8O12 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
dAURK-4 is a selective PROTAC degrader of AURKA that promotes its ubiquitination and degradation. It can be used to study glioblastoma and multiple myeloma[1][2]. It is supplied as an off-white to light yellow solid (C52H52ClFN8O12, MW 1035.47) at 99.93% purity.
Physical & Chemical Properties
| CAS Number | 2705844-81-9 |
|---|---|
| Molecular Formula | C52H52ClFN8O12 |
| Molecular Weight | 1035.47 g/mol |
| Purity | 99.93% |
| Appearance | Solid |
| 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 |
| Target | Aurora A, Cereblon |
| Signaling Pathway | Cell Cycle/DNA Damage; Epigenetics; PROTAC |
| Solubility | 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. |
| Storage | 4°C, protect from light, stored under nitrogen. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[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.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (96.57 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light, stored under nitrogen; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In MOLT-4 T-lymphoblastic leukemia cells, dAURK-4 (1 μM; 5 h) potently and selectively degrades AURKA while showing weak activity against AURKB[2]. In MM.1S multiple myeloma cells, dAURK-4 (125-1000 nM; 4-24 h) induces dose-dependent AURKA degradation, achieving nearly complete degradation at concentrations ≥250 nM[2]. In MM.1S multiple myeloma cells, dAURK-4 (0.0001-100 μM; 72 h) shows better antiproliferative activity than Alisertib, with stronger potency at low concentrations and more significant inhibition of cell viability at high concentrations[2].
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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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