Art. -Nr.: HY-135827

Roginolisib

(Synonyms: MSC2360844; IOA-244)

1 Cited Publications

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Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC₅₀ of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases.

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Reinheit: 99.66%
CAS. Nr.: 1305267-37-1
Formel: C₂₆H₂₇FN₄O₅S
Molecular Weight:526.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Roginolisib Chemical Structure

CAS. Nr.: 1305267-37-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3Kδ

145 nM (IC₅₀)

PI3Kα

18500 nM (IC₅₀)

PI3Kβ

2850 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

In Vitro

Roginolisib (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 inhibits B cell proliferation in a concentration-dependent manner with an IC₅₀ of 48 nM. Roginolisib 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.

Cell Proliferation Assay^[1]

Cell Line:

B cells
Concentration:

0-10 μM
Incubation Time:

1 hour
Result:

Inhibited B cell proliferation in a concentration-dependent manner with an IC₅₀ of 48 nM.

In Vivo

Roginolisib (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NZB/W F1 female mice^[1]
Dosage:

6.6, 22, or 66 mg/kg
Administration:

Oral; starting at week 2 post ADV-IFNα delivery, once daily at 10 weeks
Result:

Significantly reduced proteinuria incidence and severity in a dose-dependent manner.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1305267-37-1
Appearance Solid
Molecular Weight 526.58
Formel C₂₆H₂₇FN₄O₅S
Color White to off-white
SMILES

O=C(C1=NN(C2=CC=C(CN3CCOCC3)C=C2)C(C4=CC=CC(F)=C45)=C1CS5(=O)=O)N6CCOCC6
Synonyms

MSC2360844; IOA-244
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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Mol Oncol

The PI3Kδ inhibitor roginolisib (IOA-244) preserves T-cell function and activity. [Abstract]

2026 Jan 22. PMID: 41568714

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (189.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 10 mg/mL (18.99 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 10 mg/mL (18.99 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 10 mg/mL (18.99 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.8990 mL	9.4952 mL	18.9905 mL	47.4762 mL
	5 mM	0.3798 mL	1.8990 mL	3.7981 mL	9.4952 mL
	10 mM	0.1899 mL	0.9495 mL	1.8990 mL	4.7476 mL
	15 mM	0.1266 mL	0.6330 mL	1.2660 mL	3.1651 mL
	20 mM	0.0950 mL	0.4748 mL	0.9495 mL	2.3738 mL
	25 mM	0.0760 mL	0.3798 mL	0.7596 mL	1.8990 mL
	30 mM	0.0633 mL	0.3165 mL	0.6330 mL	1.5825 mL
	40 mM	0.0475 mL	0.2374 mL	0.4748 mL	1.1869 mL
	50 mM	0.0380 mL	0.1899 mL	0.3798 mL	0.9495 mL
	60 mM	0.0317 mL	0.1583 mL	0.3165 mL	0.7913 mL
	80 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5935 mL
	100 mM	0.0190 mL	0.0950 mL	0.1899 mL	0.4748 mL

Keywords

Roginolisib

1 Cited Publications

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Roginolisib

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Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Roginolisib

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Roginolisib Related Classifications

HY-135827 Related Classifications