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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- Purity: 99.80%
- CAS No.: 1621688-31-0
- 화학식: C26H27FN4O5S.1/2C4H4O4
- 분자량:584.62
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보관:
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Roginolisib hemifumarate
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Biological Activity
제품 설명
IC50 & Target
[1]|
PI3Kδ 145 nM (IC50) |
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 1621688-31-0
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Appearance Solid
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분자량 584.62
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화학식 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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Synonyms
MSC2360844 hemifumarate; IOA-244 hemifumarate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
용액&용해도
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
순도&문서
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
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 |
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| 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 |
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