NCIt definition : An orally active 2-phenylaminopyrimidine derivative with potential antineoplastic
activity. INNO-406 specifically binds to and inhibits the Bcr/Abl fusion protein tyrosine
kinase, an abnormal enzyme produced by Philadelphia chromosomal translocation associated
with chronic myeloid leukemia (CML). Furthermore, this agent also inhibits the Src-family
member Lyn tyrosine kinase, upregulated in imatinib-resistant CML cells and in a variety
of solid cancer cell types. The inhibitory effect of INNO-406 on these specific tyrosine
kinases decreases cellular proliferation and induces apoptosis. A high percentage
of CML patients are refractory to imatinib, which sometimes results from point mutations
occurring in the kinase domain of the Bcr/Abl fusion product. Due to its dual inhibitory
activity, INNO-406 has been shown to overcome this particular drug resistance and
to be a potent and effective agent in the treatment of imatinib-resistant CML.;
UNII : NVW4Z03I9B;
InChIKey : ZGBAJMQHJDFTQJ-DEOSSOPVSA-N;
CAS number : 859212-16-1; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 859212-16-1
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