Rebastinib

Rebastinib

CAT N°: 21465
Price:

From 71.00 60.35

Rebastinib is an orally bioavailable tyrosine kinase inhibitor that inhibits Abl1 (IC50 = 0.8 nM) as well as the gatekeeper mutant Abl1T315I (IC50 = 4 nM) and the activation loop mutant Abl1H396P.{34442} It also inhibits the Src family kinases Src, Lyn, Fgr, and Hck and the tyrosine kinases KDR, FLT3, and Tie2 at nanomolar concentrations. Rebastinib inhibits mutant Abl1T315I signaling and prolongs survival in a mouse Ba/F3 cell allograft model.{34442,34443} Rebastinib also exhibits in vivo antineoplastic activity against cells with the T674I point mutation of FIP1-like-1-platelet-derived growth factor receptor ?.{34444}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-[4-[[[[3-(1,1-dimethylethyl)-1-(6-quinolinyl)-1H-pyrazol-5-yl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide
  • Correlated keywords
    • DCC2036 DP1919 DP-1919 DCC-2036 abl-1 H396P T315I insert domain Tie-2 VEGFR2 VEGFR Fms Tunica interna endothelial anti-neoplastic FIP1L1 baf3 flt-3 PDGFR-a PDGFRa PDGFR?
  • Product Overview:
    Rebastinib is an orally bioavailable tyrosine kinase inhibitor that inhibits Abl1 (IC50 = 0.8 nM) as well as the gatekeeper mutant Abl1T315I (IC50 = 4 nM) and the activation loop mutant Abl1H396P.{34442} It also inhibits the Src family kinases Src, Lyn, Fgr, and Hck and the tyrosine kinases KDR, FLT3, and Tie2 at nanomolar concentrations. Rebastinib inhibits mutant Abl1T315I signaling and prolongs survival in a mouse Ba/F3 cell allograft model.{34442,34443} Rebastinib also exhibits in vivo antineoplastic activity against cells with the T674I point mutation of FIP1-like-1-platelet-derived growth factor receptor ?.{34444}

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