dAURK-4
Based on 1 Customer Validation
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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.93%
- CAS 番号: 2705844-81-9
- 分子式: C52H52ClFN8O12
- 分子量:1035.47
-
保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Cytoskeleton Compound Library
HY-L060
-
Heterocyclic Compound Library
HY-L138
-
PROTAC Library
HY-L151
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Anti-Cancer Compound Library
HY-L025
-
Autophagy Compound Library
HY-L029
-
Anti-Aging Compound Library
HY-L034
生物活性
|
Aurora A |
Cereblon |
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.
-
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 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.
化学情報
-
CAS 番号 2705844-81-9
-
性状 Solid
-
分子量 1035.47
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (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)
-
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 (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.
| 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 |
dAURK-4 関連分類
HY-137344 関連分類
Powered by Bioz