TBK1/IKKε-IN-5

CAS No. 1893397-65-3

TBK1/IKKε-IN-5( —— )

Catalog No. M21640 CAS No. 1893397-65-3

TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM respectively).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TBK1/IKKε-IN-5
  • Note
    Research use only, not for human use.
  • Brief Description
    TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM respectively).
  • Description
    TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM respectively).
  • In Vitro
    TBK1/IKKε-IN-5 (0.001-10 μM; 24 or 96 h) promotess secretion of IL-2 and IFN-γ in purified CD4+ and CD8+ T cells and IL-2 in Jurkat human T-cell leukemia cells.TBK1/IKKε-IN-5 effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects. Cell Viability Assay Cell Line:CD4+ and CD8+ T cells, Jurkat T cell leukemia cells Concentration:0.001-10 μM Incubation Time:24 h (for IL-2); 96 h(for IFN-γ)Result:Enhanced secretion of IL-2 and IFN-γ.
  • In Vivo
    TBK1/IKKε-IN-5 (40 mg/kg; p.o.; single daily for 26 days) shows good antitumor activity and prolongs survival, as well as induces immunologic memory of CT26 cells in mice when combines with anti-PD-L1. Animal Model:Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors).Dosage:40 mg/kg Administration:Oral gavage; single daily for 26 days (combine with anti-PD-L1).Result:Exhibited greater tumor control and longer survival when combined with anti-PD-L1 than used alone of both agents.Induced immunologic memory of CT26 cells in mice when combined with anti-PD-L1.
  • Synonyms
    ——
  • Pathway
    Immunology/Inflammation
  • Target
    IκB kinase (IKK)
  • Recptor
    TBK1| IKK?
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1893397-65-3
  • Formula Weight
    513.59
  • Molecular Formula
    C28H31N7O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:7.81 mg/mL (15.21 mM; Need ultrasonic)
  • SMILES
    N#Cc1cc(ccc1OC1CCOCC1)-c1ncnc(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Jenkins RW et al. Ex Vivo Profiling of PD-1 Blockade Using Organotypic Tumor Spheroids. Cancer Discov. 2018 Feb;8(2):196-215.
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