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1mg |
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5mg |
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10mg |
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Other Sizes |
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MSC2360844 is a novel, highly potent, orally bioavailable and specific PI3Kδ inhibitor with an IC50 of 145 nM. MSC2360844 shows highly specific against a panel of 278 additional kinases.
ln Vitro |
Roginolisib (0-10 μM; 1 hour) totally abolishes BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with an IC50 value of 280 nM[1]. With an IC50 of 48 nM, roginolisib suppresses B cell growth in a concentration-dependent manner. Roginolisib inhibits TLR-induced IFNα in human primary cells and BCR- and TCR-mediated responses in lymphocytes [1].
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ln Vivo |
In mouse models of SLE, roginolisib (6.6–66 mg/kg; once daily from weeks 2 to 10) improves disease expression [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: B cells Tested Concentrations: 0-10 μM Incubation Duration: 1 hour Experimental Results: Inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. |
Animal Protocol |
Animal/Disease Models: NZB/W F1 female mice [1]
Doses: 6.6, 22 or 66 mg/kg Route of Administration: oral; starting at week 2 after ADV-IFNα administration, one time/day at week 10 Experimental Results: at dose Dramatically diminished incidence and severity of proteinuria in a dependent manner. |
References |
[1]. Haselmayer P, et al. Characterization of Novel PI3Kδ Inhibitors as Potential Therapeutics for SLE and Lupus Nephritis in Pre-Clinical Studies. Front Immunol. 2014 May 22;5:233.
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Molecular Formula |
C₂₆H₂₇FN₄O₅S
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Molecular Weight |
526.58
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CAS # |
1305267-37-1
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Related CAS # |
Roginolisib hemifumarate;1621688-31-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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
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Synonyms |
MSC 2360844MSC-2360844MSC2360844IOA-244IOA 244IOA244
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~189.90 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 10 mg/mL (18.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 10 mg/mL (18.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 10 mg/mL (18.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8990 mL | 9.4952 mL | 18.9905 mL | |
5 mM | 0.3798 mL | 1.8990 mL | 3.7981 mL | |
10 mM | 0.1899 mL | 0.9495 mL | 1.8990 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.