EPZ015666

CAS No. 1616391-65-1

EPZ015666 ( EPZ-015666;GSK3235025 )

Catalog No. M12359 CAS No. 1616391-65-1

EPZ015666 (GSK3235025) is a potent, selective, orally available inhibitor of PRMT5 with Ki/IC50 of 5/22 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 50 In Stock
5MG 77 In Stock
10MG 113 In Stock
50MG 332 In Stock
100MG 478 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    EPZ015666
  • Note
    Research use only, not for human use.
  • Brief Description
    EPZ015666 (GSK3235025) is a potent, selective, orally available inhibitor of PRMT5 with Ki/IC50 of 5/22 nM.
  • Description
    EPZ015666 (GSK3235025) is a potent, selective, orally available inhibitor of PRMT5 with Ki/IC50 of 5/22 nM, displays broad selectivity against a panel of other histone methyltransferases; inhibits SmD3 methylation and causes cell death in MCL cell lines (IC50=61-904 nM), demonstrates potent concentration-dependent antiproliferative effects against Z-138 and Maver-1 cells with IC50 of 96 and 450 nM, respectively; exhibits antitumor activity in multiple MCL xenograft models.
  • Synonyms
    EPZ-015666;GSK3235025
  • Pathway
    Chromatin/Epigenetic
  • Target
    HMTase
  • Recptor
    PRMT5
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1616391-65-1
  • Formula Weight
    383.44
  • Molecular Formula
    C20H25N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO
  • SMILES
    O=C(C1=NC=NC(NC2COC2)=C1)NC[C@H](O)CN3CC4=C(C=CC=C4)CC3
  • Chemical Name
    4-Pyrimidinecarboxamide, N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-

Shipping & Storage Information

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

Reference

1. Chan-Penebre E, et al. Nat Chem Biol. 2015 Jun;11(6):432-7.
2. Kryukov GV, et al. Science. 2016 Mar 11;351(6278):1214-8.
3. Chan-Penebre E, et al. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6.
4. Gullà A, et al. Leukemia. 2018 Apr;32(4):996-1002.
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