IPI-549

Igoa vaila'au:

(S)-2-amino-N-(1-(8-((1-methyl-1H-pyrazol-4-yl) ethynyl)-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl )ethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

SMILES Code:

O=C(C1=C2N=CC=CN2N=C1N)N[C@H](C3=CC4=C(C(N3C5=CC=CC=C5)=O)C(C#CC6=CN(C) N=C6)=CC=C4)C

InChi Code:

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

InChi Key:

XUMALORDVCFWKV-IBGZPJMESA-N

upu autu:

IPI-549, IPI 549, IPI549, 1693758-51-8

Solubility:Solu i le DMSO

Teuina:0 - 4°C mo taimi pupuu (aso i vaiaso), poo le -20°C mo taimi uumi (masina).

Fa'amatalaga:

IPI-549 faʻalavelave PI3Kγ ma IC50 o 16 nM, faʻatasi ai ma> 100-filifili filifili i luga o isi lipid ma protein kinases (PI3Kα IC50 = 3.2 μM, PI3Kβ IC50 = 3.5 μM, PI3Kδ IC50> 8.4 μM). IPI549 e su'esu'eina mo gaioiga i va'aiga uma o Vasega I PI3K isoforms. O le sootaga vavalalata o le IPI549 mo le PI3K-γ e faʻamoemoeina e ala i le fuaina o fua faatatau taʻitasi ma mo le PI3K-α, β ma le δ e faʻaaoga ai le paleni fluorescent titration. IPI549 o loʻo maua o se faʻamaufaʻailoga mataʻina i le PI3Kγ faʻatasi ai ma le Kd o le 290 pM ma> 58-gaeleele vaivai affinity mo isi Vasega I PI3K isoforms (PI3Kα Kd = 17 nM, PI3Kβ Kd = 82 nM, PI3Kδ Kd = 23 M). I le PI3K-α, -β, -γ, ma le -δ faʻalagolago ile cellular phospho-AKT assays, IPI549 faʻaalia PI3K-γ malosi sili (IC50 = 1.2 nM) ma le filifilia e faasaga i isi Vasega I PI3K isoforms (> 146-fold). Cellular IC50s mo Vasega I PI3Kα (250 nM), PI3Kβ (240 nM), PI3Kγ (1.2 nM), PI3Kδ (180 nM) e faʻamoemoeina ile SKOV-3, 786-O, RAW 264.7, ma le RAJI sela, i le faasologa, e ala i le mataʻituina. taofia o pAKT S473 e ELISA. E le gata i lea, o le fua ole IPI549 e fa'alagolago e taofia ai le PI3Kγ fa'alagolago ile macrophage (BMDM) fa'alagolago ile ponaivi. IPI549 o loʻo maua foi e filifili e faasaga i se laulau o 80 GPCRs, laina ion, ma felauaiga i le 10 μM [1].

Sini: PI3Kγ,PI3Kβ