P21d hydrochloride: R&D Systems
Catalog Number: 6073
Chemical Name: [4-[[6-Cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-fluorophenyl]-4-morpholinylmethanone hydrochloride
Biological Activity
Potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B kinase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also active in vivo and orally bioavailable.
Technical Data
  • M.Wt:
    483.93
  • Formula:
    C23H22FN7O2.HCl
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.
    Zeng et al.
    Bioorg.Med.Chem.Lett, 2011;21:5870
  2. PTK6 inhibition suppresses metastases of triple-negative breast cancer via SNAIL-dependent E-cadherin regulation.
    Ito et al.
    Cancer Res., 2016;76:4406
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