Deskrizzjoni
Struttura Kimika: IPI-549
Nru CAS: 1693758-51-8
IPI-549(IPI549;Eganelisib)
Katalgu Nru.: URK-V596Użat biss għal-laboratorju.
Eganelisib (IPI-549) is a potent, highly selective, orally active inhibitor of PI3Kγ with IC50 of 16 nM, displays >100-fold selectivity over other lipid and protein kinases (PI3Kα IC50=3.2 uM, PI3Kβ IC50=3.5 uM, PI3Kδ IC50>8.4 uM).
Attività Bijoloġika
Eganelisib (IPI-549) is a potent, highly selective, orally active inhibitor of PI3Kγ with IC50 of 16 nM, displays >100-fold selectivity over other lipid and protein kinases (PI3Kα IC50=3.2 uM, PI3Kβ IC50=3.5 uM, PI3Kδ IC50>8.4 uM).
Eganelisib (IPI-549) demonstrates excellent PI3Kγ potency (IC50=1.2 nM) and selectivity against other Class I PI3K isoforms (>146-darbiet) f'assaġġi ta' fosfo-AKT ċellulari, jinibixxi l-migrazzjoni tal-makrofagi derivati mill-mudullun (BMDM) dipendenti fuq PI3K.
Eganelisib (IPI-549) juri proprjetajiet farmakokinetiċi favorevoli u inibizzjoni robusta tal-migrazzjoni tan-newtrofili medjata minn PI3K in vivo.
Proprjetajiet fiżikokimiċi
|
M.Wt |
528.564 |
|
|
Formula |
C30H24N8O2 |
|
|
CAS Nru. |
1693758-51-8 |
|
|
Ħażna |
Trab solidu -20 grad 3years; 4 grad 2 snin |
Fis-Solvent -80 grad 6 Xhur -20 grad 1 Xahar |
|
Solubilità |
15 mM f'DMSO |
|
|
Isem Kimiku |
Pyrazolo[1,5-a]pyrimidine-3-carboxamide,2-amino-N-[(1S)-1-[1,2-dihydro{{10} }[2-({1-metil-1H-pirazol-4-il)etinil]-1-oxo-2-fenil-3-isoquinolinyl] etil]- |
|
Referenzi
1. Evans CA, et al. ACS Med Chem Lett. 2016 Lulju 22;7(9):862-7.
2. De Henau O, et al. Natura. 2016 Nov 17;539(7629):443-447.
URK-V596_COAURK-V596_SDSURK-V596_TDSNota: Il-prodotti kollha ta 'Ureiko jintużaw biss għal riċerka xjentifika jew dikjarazzjoni ta' ċertifikat tad-droga, u aħna ma nipprovdux prodotti u servizzi għal kwalunkwe użu personali!
It-tags Popolari: ipi549 kas nr.: 1693758-51-8
Ibgħat l-inkjesta
Tista 'Tħobb ukoll
