IPI-549
Lintlha tsa Sehlahisoa
Li-tag tsa Sehlahisoa
| Boholo ba Pakete | Ho fumaneha | Theko (USD) |
| 100mg | E teng thepeng e teng ka lebenkeleng | 500 |
| 250mg | E teng thepeng e teng ka lebenkeleng | 950 |
| 500mg | E teng thepeng e teng ka lebenkeleng | 1300 |
| 1g | E teng thepeng e teng ka lebenkeleng | 1700 |
| Boholo bo Eketsehileng | Fumana Litlhaloso | Fumana Litlhaloso |
Lebitso la lik'hemik'hale:
(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 Khouto:
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
Khoutu ea 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
InChi Key:
XUMALORDVCFWKV-IBGZPJMESA-N
Keyword:
IPI-549, IPI 549, IPI549, 1693758-51-8
Sollubility:E qhibiliha ka DMSO
Polokelo:0 - 4 ° C bakeng sa nako e khutšoanyane (matsatsi ho isa libeke), kapa -20 ° C bakeng sa nako e telele (likhoeli).
Tlhaloso:
IPI-549 e thibela PI3Kγ e nang le IC50 ea 16 nM, e nang le> khetho ea 100 ka makhetlo a mangata holim'a lipid le protheine kinases (PI3Kα IC50 = 3.2 μM, PI3Kβ IC50 = 3.5 μM, PI3Kδ IC50> 8.4 μM). IPI549 e ea hlahlojoa bakeng sa ts'ebetso ho li-isoform tsohle tsa Sehlopha sa I PI3K. Kamano e tlamang ea IPI549 bakeng sa PI3K-γ e khethoa ka ho lekanya litekanyetso tsa motho ka mong le bakeng sa PI3K-α, β le δ ho sebelisa equilibrium fluorescent titration. IPI549 e fumanoa e le tlamahano e thata ka mokhoa o makatsang ho PI3Kγ e nang le Kd ea 290 pM le > 58-fold affinity e fokolang bakeng sa li-isoform tse ling tsa Sehlopha sa I PI3K (PI3Kα Kd=17 nM, PI3Kβ Kd=82 nM, PI3Kδ Kd=23 M). Litlhahlobong tsa PI3K-α, -β, -γ, le -δ tse itšetlehileng ka cellular phospho-AKT, IPI549 e bontša potency e babatsehang ea PI3K-γ (IC50 = 1.2 nM) le khetho khahlanong le li-isoforms tse ling tsa Sehlopha sa I PI3K (> 146-fold). Li-Cellular IC50s bakeng sa Sehlopha sa I PI3Kα (250 nM), PI3Kβ (240 nM), PI3Kγ (1.2 nM), PI3Kδ (180 nM) li khethoa ho SKOV-3, 786-O, RAW 264.7, le RAJI ka lisele, ka ho latellana, ka ho latellana, ka ho latellana. thibelo ea pAKT S473 ka ELISA. Ho feta moo, IPI549 tekanyo e itšetlehileng ka eona e thibela ho falla ha PI3Kγ e itšetlehileng ka moko oa macrophage (BMDM). IPI549 e boetse e fumanoa e le khetho khahlanong le sehlopha sa 80 GPCRs, mechine ea ion, le lipalangoang ho 10 μM[1].
Sepheo: PI3Kγ,PI3Kβ
