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IPI-145 (INK1197)PI3K-δ/PI3K-γ inhibitor

IPI-145 (INK1197)

Catalog No. A1720
Size Price Stock Qty
10mM (in 1mL DMSO) $88.00 In stock
5mg $80.00 In stock
10mg $110.00 In stock
50mg $210.00 In stock
100mg $260.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

IPI-145 (INK1197)

Biological Activity

Description IPI-145 is an orally bioavailable and highly selective inhibitor of PI3K-δ and PI3K-γ with IC50 values of 0.36 nM and 19.6 nM, respectively.
Targets PI3K-δ PI3K-γ        
IC50 0.36 nM 19.6 nM        

Protocol

Cell experiment [1]:

Cell lines

Primary B cells and primary T cells

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.

Reacting condition

IC50 value : 0.5 or 9.5 nM

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]:

Animal models

Rats with previously established air pouches

Dosage form

1, 2.5, 5 and 10 mg/kg; p.o.

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.

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.

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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Chemical Properties

Cas No. 1201438-56-3 SDF Download SDF
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 >20.8mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.