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Version: 17.08d (Release date: 2017-08-28)
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Bafetinib (Code C62516)

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Terms & Properties

Preferred Name: Bafetinib

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.

Display Name: Bafetinib

Label: Bafetinib

NCI Thesaurus Code: C62516 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C2607225  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Benzamide, N-[3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl]-4-[[(3S)-3- (dimethylamino)-1-pyrrolidinyl]methyl]-3-(trifluoromethyl)-
Dual Bcr-Abl/Lyn Tyrosine Kinase Inhibitor INNO-406

External Source Codes: 
CAS Registry Number 859212-16-1 (see NLM ChemIDplus info)
PDQ Closed Trial Search ID 500041
PDQ Open Trial Search ID 500041 (check for NCI PDQ open clinical trial info)
UMLS CUI C2607225

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C30H31F3N8O
code C62516
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name INNO-406
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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