MS44
MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand.
(Pink: Aurora B ligand (HY-175526); Blue: VHL ligand (HY-112078); Black: linker).
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- 純度: 99.81%
- 分子式: C57H72FN11O8S
- 分子量:1090.31
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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
生物活性
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Aurora B 103 nM (DC50) |
VHL |
MS44 (Compound 18) (1 nM-10 μM, 1-96 h) effectively degrades AURKB in a concentration- and time-dependent manner in HPAF-11 cells by hijacking the UPS and also in multiple cancer cell lines[1].
MS44 (1 μM, 24-96 h) inhibits the proliferation in HPAF-11, K562, U937, CFPAC-1, SW1783 and HT-29 cells[1].
MS44 (48 h) induces U937 cells G2/M arrest[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HPAF-11 cells, K562 cells and U937 cells
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Concentration:1 μM
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Incubation Time:24, 48, 72 and 96 h
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Result:Effectively suppressed the proliferation of HPAF-11 cells.
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Cell Line:HPAF-11, K562, U937, CFPAC-1, SW1783 and HT-29 cells
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Concentration:1, 3, 10, 30, 100, 300 nM, 1, 3, 10 μM for HPAF-11 and 1 μM for other cells
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Incubation Time:1, 2, 4, 8, 12, and 24 h for HPAF-11 and 24 h for other cells
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Result:Induced significant degradation of AURKB in all cells.
Degraded AURKB in a concentration- and time-dependent manner in HPAF-11 cells by hijacking the UPS.
Selectively degraded AURKB over AURKA and AURKC in HPAF-11 cells.
化学情報
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性状 Solid
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分子量 1090.31
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分子式 C57H72FN11O8S
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Color White to off-white
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCCCC(N(CCCOC4=CC5=NC=NC(NC6=NNC(CC(NC7=CC=CC(F)=C7)=O)=C6)=C5C=C4)CCO)=O)=O)=O)O)=O)C
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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
DMSO : 100 mg/mL (91.72 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)
純度とドキュメンテーション
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データシート (270 KB)
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SDS (252 KB)
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- Portuguese - PT (252 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9172 mL | 4.5859 mL | 9.1717 mL | 22.9293 mL |
| 5 mM | 0.1834 mL | 0.9172 mL | 1.8343 mL | 4.5859 mL | |
| 10 mM | 0.0917 mL | 0.4586 mL | 0.9172 mL | 2.2929 mL | |
| 15 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5286 mL | |
| 20 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1465 mL | |
| 25 mM | 0.0367 mL | 0.1834 mL | 0.3669 mL | 0.9172 mL | |
| 30 mM | 0.0306 mL | 0.1529 mL | 0.3057 mL | 0.7643 mL | |
| 40 mM | 0.0229 mL | 0.1146 mL | 0.2293 mL | 0.5732 mL | |
| 50 mM | 0.0183 mL | 0.0917 mL | 0.1834 mL | 0.4586 mL | |
| 60 mM | 0.0153 mL | 0.0764 mL | 0.1529 mL | 0.3822 mL | |
| 80 mM | 0.0115 mL | 0.0573 mL | 0.1146 mL | 0.2866 mL |