2. PI3K/Akt/mTOR
  3. PI3K
  4. Roginolisib hemifumarate

Roginolisib hemifumarate  (Synonyms: MSC2360844 hemifumarate; IOA-244 hemifumarate)

Cat. No.: HY-135827A Purity: 99.95%
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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.

For research use only. We do not sell to patients.

Roginolisib hemifumarate Chemical Structure

Roginolisib hemifumarate Chemical Structure

CAS No. : 1621688-31-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
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Solid
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10 mg USD 385 In-stock
25 mg USD 750 In-stock
50 mg USD 1200 In-stock
100 mg USD 1900 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Roginolisib hemifumarate:

Roginolisib hemifumarate Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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.

Roginolisib hemifumarate Related Antibodies

Cell Viability 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 hemifumarate (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.
Molecular Weight

584.62

Formula

C26H27FN4O5S.1/2C4H4O4
CAS No.
Appearance

Solid

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.OC(/C=C/C(O)=O)=O.[1/2]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7105 mL 8.5526 mL 17.1051 mL
5 mM 0.3421 mL 1.7105 mL 3.4210 mL
View the 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.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
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
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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Roginolisib hemifumarate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Roginolisib hemifumarate1621688-31-0MSC2360844 hemifumarateIOA-244 hemifumaratePI3KPhosphoinositide 3-kinaseBcellsSLE-pronefunctionsproliferationprimaryInhibitorinhibitorinhibit

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