Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ, more than 100 times more selective than other lipid and protein kinases. Biochemical IC50 was 16 nM.

 

Brand: BCM

 

Target: PI3K

 

Signaling Pathways: PI3K/Akt/mTOR signaling

 

In Vitro: IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells.

 

In Vivo: IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo.

 

pKa: 10.81±0.46(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

Isomeric SMILES: C[C@@H](C1=CC2=C(C(=CC=C2)C#CC3=CN(N=C3)C)C(=O)N1C4=CC=CC=C4)NC(=O)C5=C6N=CC=CN6N=C5N  

 

InChIKey: XUMALORDVCFWKV-IBGZPJMESA-N  

 

InChI: InChI=1S/C30H24N8O2/c1-19(34-29(39)26-27(31)35-37-15-7-14-32-28(26)37)24-16-22-9-6-8-21(13-12-20-17-33-36(2)18-20)25(22)30(40)38(24)23-10-4-3-5-11-23/h3-11,14-19H,1-2H3,(H2,31,35)(H,34,39)/t19-/m0/s1

 

Attribute
[Chem Name]	2-amino-N-[(1S)-1-[8-[2-(1-methylpyrazol-4-yl)ethynyl]-1-oxo-2-phenylisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
[CAS No.]	1693758-51-8
[MDL No.]	MFCD30533720
[Formula]	C30H24N8O2
[Molecular]	528.56
[Form]	Pale yellow powder
[Storage]	Keep in dark place. Inert atmosphere, 2-8°C
[Synonym]	IPI-549; Eganelisib

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