IPI-549

Chemical Name:

(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 Kodhi:

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

Keyword:

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

Solubility:Soluble muDMSO

Kuchengeta:0 - 4 ° C kwenguva pfupi (mazuva kusvika mavhiki), kana -20 ° C kwenguva refu (mwedzi).

Tsanangudzo:

IPI-549 inhibits PI3Kγ ne IC50 ye16 nM, ine > 100-fold selectivity pane mamwe lipid uye protein kinases (PI3Kα IC50 = 3.2 μM, PI3Kβ IC50 = 3.5 μM, PI3Kδ IC50> 8.4 μM). IPI549 inoongororwa chiitiko kune ese Kirasi I PI3K isoforms. Kubatana kunosunga kweIPI549 kwePI3K-γ kunotsanangurwa nekuyera mareti ega ega uye yePI3K-α, β uye δ uchishandisa equilibrium fluorescent titration. IPI549 inowanikwa iri bhainda rinoshamisa kuPI3Kγ ine Kd ye290 pM uye > 58-yakapetwa isina kusimba kune mamwe Class I PI3K isoforms (PI3Kα Kd=17 nM, PI3Kβ Kd=82 nM, PI3Kδ Kd=23 M). MuPI3K-α, -β, -γ, uye -δ inotsamira cellular phospho-AKT assays, IPI549 inoratidza yakanakisa PI3K-γ potency (IC50=1.2 nM) uye selectivity kurwisa mamwe Kirasi I PI3K isoforms (> 146-fold). Cellular IC50s yeKirasi I PI3Kα (250 nM), PI3Kβ (240 nM), PI3Kγ (1.2 nM), PI3Kδ (180 nM) inotemerwa muSKOV-3, 786-O, RAW 264.7, uye RAJI nemaseru, zvichiteerana, zvichiteerana inhibition yepAKT S473 by ELISA. Uyezve, IPI549 dose dependently inhibits PI3Kγ inotsamira pfupa-inotorwa macrophage (BMDM) kutama. IPI549 inowanikwawo inosarudza pakatarisana nepaneru ye80 GPCRs, ion nzira, uye vatakuri pa10 μM[1].

Chinangwa: PI3Kγ,PI3Kβ