IPI-549

IPI-549
  • Name: IPI549
  • Catalog No.: CPD1022
  • CAS No.: 1693758-51-8
  • Molecular Weight: 528.56
  • Chemical Formula: C30H24N8O2
  • For scientific research only, not for patients.

    Product Detail

    Product Tags

    Pack Size Availability Price (USD)
    100mg In stock 500
    250mg In stock 950
    500mg In stock 1300
    1g In stock 1700
    More Sizes Get Quotes Get Quotes

    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 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

    Keyword:

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

    Solubility: Soluble in DMSO

    Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months).

    Description: 

    IPI-549 inhibits PI3Kγ with IC50 of 16 nM, with >100-fold selectivity over other lipid and protein kinases (PI3Kα IC50=3.2 μM, PI3Kβ IC50=3.5 μM, PI3Kδ IC50>8.4 μM). IPI549 is evaluated for activity across all Class I PI3K isoforms. The binding affinity of IPI549 for PI3K-γ is determined by measuring the individual rates constants and for PI3K-α, β and δ using equilibrium fluorescent titration. IPI549 is found to be a remarkably tight binder to PI3Kγ with a Kd of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms (PI3Kα Kd=17 nM, PI3Kβ Kd=82 nM, PI3Kδ Kd=23 M). In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, IPI549 demonstrates excellent PI3K-γ potency (IC50=1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold). Cellular IC50s for Class I PI3Kα (250 nM), PI3Kβ (240 nM), PI3Kγ (1.2 nM), PI3Kδ (180 nM) are determined in SKOV-3, 786-O, RAW 264.7, and RAJI cells, respectively, by monitoring inhibition of pAKT S473 by ELISA. Furthermore, IPI549 dose dependently inhibits PI3Kγ dependent bone marrow-derived macrophage (BMDM) migration. IPI549 is also found to be selective against a panel of 80 GPCRs, ion channels, and transporters at 10 μM[1].

    Target: PI3Kγ,PI3Kβ




  • Previous:
  • Next:

  • Related Products

    
    WhatsApp Online Chat !