GNE-431

CAS No. 1433820-83-7

GNE-431( GNE431 )

Catalog No. M11843 CAS No. 1433820-83-7

GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GNE-431
  • Note
    Research use only, not for human use.
  • Brief Description
    GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively.
  • Description
    GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively; shows higher selectivity for Btk than any of the covalent inhibitors or non-covalent analogs profiled; does not interact with Cys481 and differs from covalent inhibitors like ibrutinib, potently inhibits the ibrutinib-resistant Btk C481S mutant in vitro and in cells; also shows excellent potency against the C481R, T474I, and T474M mutants (IC50=7.5-10 nM); potently inhibits BCR signaling in stimulated human blood and blocks Btk autophosphorylation in C481S-transfected cells.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    GNE431
  • Pathway
    Tyrosine Kinase
  • Target
    BTK
  • Recptor
    BTK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1433820-83-7
  • Formula Weight
    564.654
  • Molecular Formula
    C30H32N10O2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C1N(C2=NC=CC(C3=NN4C=CN=C4C(NC(C=C5C6)=NN5CCN6C)=C3)=C2CO)CCN7C1=CC8=C7CCCC8
  • Chemical Name
    3,4,6,7,8,9-Hexahydro-2-[3-(hydroxymethyl)-4-[8-[(4,5,6,7-tetrahydro-5-methylpyrazolo[1,5-a]pyrazin-2-yl)amino]imidazo[1,2-b]pyridazin-6-yl]-2-pyridinyl]pyrazino[1,2-a]indol-1(2H)-one

Shipping & Storage Information

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

Reference

1. Johnson AR, et al. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907.
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