Roginolisib hemifumarate
Based on 1 publication(s) in Google Scholar
Roginolisib (MSC2360844) hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib hemifumarate shows highly selective against a panel of 278 additional kinases.
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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: 99.80%
- CAS 番号: 1621688-31-0
- 分子式: C26H27FN4O5S.1/2C4H4O4
- 分子量:584.62
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Roginolisib hemifumarate
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生物活性
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PI3Kδ 145 nM (IC50) |
Roginolisib hemifumarate (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC50 values of 280 nM[1].
Roginolisib hemifumarate inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. Roginolisib hemifumarate blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B cells
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Concentration:0-10 μM
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Incubation Time:1 hour
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Result:Inhibited B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NZB/W F1 female mice[1]
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Dosage:6.6, 22, or 66 mg/kg
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Administration:Oral; starting at week 2 post ADV-IFNα delivery, once daily at 10 weeks
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Result:Significantly reduced proteinuria incidence and severity in a dose-dependent manner.
化学情報
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CAS 番号 1621688-31-0
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性状 Solid
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分子量 584.62
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分子式 C26H27FN4O5S.1/2C4H4O4
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Color White to off-white
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SMILES
O=C(C1=NN(C2=CC=C(CN3CCOCC3)C=C2)C(C4=CC=CC(F)=C45)=C1CS5(=O)=O)N6CCOCC6.OC(/C=C/C(O)=O)=O
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別名
MSC2360844 hemifumarate; IOA-244 hemifumarate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Oncol
2026 Jan 22. PMID: 41568714
溶剤 & 溶解度
DMSO : 100 mg/mL (171.05 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (280 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 (sealed storage, away from moisture). 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 | 1.7105 mL | 8.5526 mL | 17.1051 mL | 42.7628 mL |
| 5 mM | 0.3421 mL | 1.7105 mL | 3.4210 mL | 8.5526 mL | |
| 10 mM | 0.1711 mL | 0.8553 mL | 1.7105 mL | 4.2763 mL | |
| 15 mM | 0.1140 mL | 0.5702 mL | 1.1403 mL | 2.8509 mL | |
| 20 mM | 0.0855 mL | 0.4276 mL | 0.8553 mL | 2.1381 mL | |
| 25 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7105 mL | |
| 30 mM | 0.0570 mL | 0.2851 mL | 0.5702 mL | 1.4254 mL | |
| 40 mM | 0.0428 mL | 0.2138 mL | 0.4276 mL | 1.0691 mL | |
| 50 mM | 0.0342 mL | 0.1711 mL | 0.3421 mL | 0.8553 mL | |
| 60 mM | 0.0285 mL | 0.1425 mL | 0.2851 mL | 0.7127 mL | |
| 80 mM | 0.0214 mL | 0.1069 mL | 0.2138 mL | 0.5345 mL | |
| 100 mM | 0.0171 mL | 0.0855 mL | 0.1711 mL | 0.4276 mL |
Roginolisib hemifumarate 関連分類
HY-135827A 関連分類
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