page_title: Bafetinib
section_title: Binding
hierarchical_section_title: Bafetinib / Development / Binding
caption_attribution_description: English: Bafetinib in it's binding site. Amino acids with major interactions displayed, dotted lines represent hydrogen bonds.
context_page_description: Bafetinib is an experimental cancer drug developed by Nippon Shinyaku and licensed to CytRx. It is an inhibitor of Lyn and Bcr-Abl. It reached phase II clinical trials in 2010.
context_section_description: Due to the structural similarities of imatinib and bafetinib, their binding to Bcr-Abl is also quite similar. The only notable difference comes from the hydrophobic interaction between the trifluoromethyl group and the hydrophobic pocket created by Ile-293, Leu-298, Leu-354, and Val-379. This group can also be linked to bafetinib's specificity for Lyn, as the binding site there is almost identical to that on Bcr-Abl.
  Bafetinib is effective both against most imatinib resistant mutations (not including T315I) and some dasatinib resistant mutations. Bafetinib also has more affinity for Bcr-Abl than nilotinib (but less than dasatinib) but only targets Bcr-Abl and Src family kinases Lck and Lyn; with unrivalled specificity which suggests the probability of fewer adverse effects.
caption: Bafetinib in its binding site
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