GSK2879552 dihydrochloride

CAS No. 1902123-72-1

GSK2879552 dihydrochloride( ——— )

Catalog No. M38014 CAS No. 1902123-72-1

GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GSK2879552 dihydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
  • Description
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
  • In Vitro
    Cell Viability Assay.Cell Line:9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. Concentration:0-10000 nM.Incubation Time:6 days.Result:Inhibited cell proliferation.RT-PCR.Cell Line:Resistant HCC cells (PLC/PRF/5 and Huh7). Concentration:0, 1, 2 μM.Incubation Time:24 h.Result:Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9,Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.
  • In Vivo
    Animal Model:NCI-H526 and NCI-H1417 xenografts.Dosage:1.5 mg/kg.Administration:PO daily for 25-35 days.Result:There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.
  • Synonyms
    ———
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    KDM1/LSD1
  • Research Area
    ———
  • Indication
    ———

Chemical Information

  • CAS Number
    1902123-72-1
  • Formula Weight
    437.4
  • Molecular Formula
    C23H30Cl2N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    H2O : 100 mg/mL (228.62 mM) DMSO : 31.25 mg/mL (71.44 mM)
  • SMILES
    ———
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Huang M, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Apr 2;398:12-21.?
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