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GSK3368715 dihydrochloride

CAS No. 1628925-77-8

GSK3368715 dihydrochloride( —— )

Catalog No. M32952 CAS No. 1628925-77-8

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GSK3368715 dihydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8.
  • Description
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • In Vitro
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types.
  • In Vivo
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Histone Methyltransferase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1628925-77-8
  • Formula Weight
    439.46
  • Molecular Formula
    C20H40Cl2N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 230 mg/mL (523.37 mM; Ultrasonic ) H2O : 140 mg/mL (318.57 mM; Ultrasonic)
  • SMILES
    Cl.Cl.CCOCC1(COCC)CCC(CC1)c1n[nH]cc1CN(C)CCNC
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.?
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