GDC-0941 (Pictilisib)Catalog No. A10421

Quick Overview

GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) , with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR respectively.
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GDC-0941 (Pictilisib)

GDC-0941 (Pictilisib)  Citations(2)
  • Li T,et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 30013190
  • Joo Sang Lee,et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 29959327
  • Product Information
    Catalog Num A10421
    M. Wt 513.6
    Formula C23H27N7O3S2
    Solubility DMSO
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 957054-30-7
    Synonyms GDC0941
    Chemical Name 2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine
    SMILES Code CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6

    Biological activity
    Introduction
    GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) , with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR respectively.
    Targets
    Target Value
    p110αIC50: 3nM
    p110δIC50: 3nM
    p110βIC50: 33nM
    p110γIC50: 75nM
    mTORKiapp0.58μM
    C2βIC50: 0.67μM
    DNA-PKIC50: 1.23μM
    Vps34IC50: >10μM
    Solubility
    Solubility (25C) * In vitro DMSO 44 mg/mL (85.66 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80 30 mg/mL
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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    High Purity Kinase Inhibitors on Signaling Pathways

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