RO5454948
Based on 1 publication(s) in Google Scholar
RO5454948 (Compound 9) is the inhibitor for Dyrk1B and Dyrk1A with IC50 of 68 nM and 22 nM. RO5454948 exhibits cytotoxicity in cancer cell SW620 with EC50 of 1.9 μM.
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- 純度: 99.53%
- CAS 番号: 1386979-55-0
- 分子式: C23H17Cl2N5O4
- 分子量:498.32
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 RO5454948
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生物活性
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DYRK1A 22 nM (IC50) |
DYRK1B 68 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW-620 | EC50 |
1.9 μM
Compound: 9
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Cytotoxicity against human SW620 cells
Cytotoxicity against human SW620 cells
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[PMID: 24239188] |
RO5454948 (0-2.5 μM, 48 h) promotes cancer cells to enter the cell cycle from the quiescent phase, stimulates the generation of ROS, induces DNA damage and apoptosis in cancer cell Panc1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc1
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Concentration:0-2.5 μM
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Incubation Time:48 h
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Result:Increased expression of cleaved PARP and γH2AX.
化学情報
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CAS 番号 1386979-55-0
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性状 Solid
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分子量 498.32
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分子式 C23H17Cl2N5O4
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Color White to off-white
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SMILES
ClC1=CC=C(C(NCC2=CC(Cl)=CC=C2)=O)C=C1NC(C3=CC4=CN=C(OC)N=C4N=C3O)=O
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別名
Mirk-IN-1; Dyrk1B/A-IN-1
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Biol Res
DYRK1-mediated phosphorylation of endocytic components is required for extracellular lumen expansion in ascidian notochord. [Abstract]2023 Mar 11;56(1):10. PMID: 36899423
溶剤 & 溶解度
DMSO : 2 mg/mL (4.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ewton DZ, et al. Inactivation of mirk/dyrk1b kinase targets quiescent pancreatic cancer cells. Mol Cancer Ther. 2011 Nov;10(11):2104-14. [Content Brief]
[2]. Anderson K, et al. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. [Content Brief]
[3]. Deng X, et al., Mirk kinase inhibition blocks the in vivo growth of pancreatic cancer cells. Genes Cancer. 2014 Sep;5(9-10):337-47. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0067 mL | 10.0337 mL | 20.0674 mL | 50.1686 mL |