Bafetinib

Bafetinib

CAT N°: 19169
Price:

From 66.00 56.10

Bcr-Abl, a fusion protein with deregulated tyrosine kinase activity, is highly expressed in chronic myelogenous leukemia (CML). Bafetinib is a rationally developed tyrosine kinase inhibitor based on the chemical structure of imatinib (Item No. 13139), with modifications added to improve binding and potency against Bcr-Abl kinase (IC50 = 5.8 nM).{30982} It is 25- to 55-fold more potent than imatinib in vitro and ?10-fold more potent in vivo.{30982} Bafetinib inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation and also targets the Src family kinase Lyn (IC50 = 19 nM), which has been associated with resistance to imatinib in CML.{30982}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[3-([4,5′-bipyrimidin]-2-ylamino)-4-methylphenyl]-4-[[(3S)-3-(dimethylamino)-1-pyrrolidinyl]methyl]-3-(trifluoromethyl)-benzamide
  • Correlated keywords
    • Inno406 NS187 CNS9 CNS09 CNS-9 BCR-Abl BCRAbl bcrabl bcr-abl CMLlyn T315I Src CNS-09
  • Product Overview:
    Bcr-Abl, a fusion protein with deregulated tyrosine kinase activity, is highly expressed in chronic myelogenous leukemia (CML). Bafetinib is a rationally developed tyrosine kinase inhibitor based on the chemical structure of imatinib (Item No. 13139), with modifications added to improve binding and potency against Bcr-Abl kinase (IC50 = 5.8 nM).{30982} It is 25- to 55-fold more potent than imatinib in vitro and ?10-fold more potent in vivo.{30982} Bafetinib inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation and also targets the Src family kinase Lyn (IC50 = 19 nM), which has been associated with resistance to imatinib in CML.{30982}

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