IPI-145 (INK1197) (Synonyms: Duvelisib, INK1197) |
| Catalog No.GC10749 |
IPI-145 (INK1197) (IPI-145) is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1201438-56-3
Sample solution is provided at 25 µL, 10mM.
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IPI-145 (also known as INK1197), an isoquinolinone derivative, is a small-molecule phosphoinositide-3 kinases (PI3K) inhibitor that selectively and potently inhibits two PI3K isoforms, PI3K-δ and PI3K-γ, with half maximal inhibition concentration IC50 of 2.5 nM and 27 nM respectively. Despite of preference for PI3K-δ and PI3K-γ, IPI-145 also inhibits other PI3K isoforms, PI3K-α and PI3K-β, to a lesser extent with IC50 of 1602 nM and 85 nM respectively.
Due to the essential role of PI3K-δ in the proliferation of B cell and T cell, IPI-145 exhibits potent anti-proliferative activity against both cells with IC50 of 0.5 nM and 9.5 nM respectively leading to inhibition of neutrophil migration and basophil activation.
Inhibition of immune function through IPI-145-induced PI3K-δ and PI3K-γ blockade potentiates its application in the treatment of multiple inflammatory, autoimmune and hematologic diseases.
References:
[1] Winkler DG1, Faia KL, DiNitto JP, Ali JA, White KF, Brophy EE, Pink MM, Proctor JL, Lussier J, Martin CM, Hoyt JG, Tillotson B, Murphy EL, Lim AR, Thomas BD, Macdougall JR, Ren P, Liu Y, Li LS, Jessen KA, Fritz CC, Dunbar JL, Porter JR, Rommel C, Palombella VJ, Changelian PS, Kutok JL. PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. doi: 10.1016/j.chembiol.2013.09.017. Epub 2013 Nov 7.
| Cell experiment [1]: | |
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Cell lines |
Primary B cells and primary T cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
IC50 value : 0.5 or 9.5 nM |
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Applications |
IPI-145 showed potent anti-proliferative activity against both primary B cells and primary T cells, with IC50 values of 0.5 nM and 9.5 nM, respectively. Thus, it inhibited neutrophil migration and basophil activation. |
| Animal experiment [1]: | |
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Animal models |
Rats with previously established air pouches |
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Dosage form |
1, 2.5, 5 and 10 mg/kg; p.o. |
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Applications |
At the doses of 5 and 10 mg/kg, IPI-145 significantly inhibited neutrophil migration. More specifically, in the 10 mg/kg dose group, all animals showed significantly decreased neutrophil migration. In the 5 and 2.5 mg/kg dose groups, the results were more variable. The animals treated with 1 mg/kg IPI-145 showed little inhibition. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Winkler DG1, Faia KL, DiNitto JP, Ali JA, White KF, Brophy EE, Pink MM, Proctor JL, Lussier J, Martin CM, Hoyt JG, Tillotson B, Murphy EL, Lim AR, Thomas BD, Macdougall JR, Ren P, Liu Y, Li LS, Jessen KA, Fritz CC, Dunbar JL, Porter JR, Rommel C, Palombella VJ, Changelian PS, Kutok JL. PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. |
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| Cas No. | 1201438-56-3 | SDF | |
| Synonyms | Duvelisib, INK1197 | ||
| Chemical Name | 8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one | ||
| Canonical SMILES | CC(C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5 | ||
| Formula | C22H17ClN6O | M.Wt | 416.86 |
| Solubility | ≥ 20.843mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3989 mL | 11.9944 mL | 23.9889 mL |
| 5 mM | 0.4798 mL | 2.3989 mL | 4.7978 mL |
| 10 mM | 0.2399 mL | 1.1994 mL | 2.3989 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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