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Version: 16.11d (Release date: 2016-11-28)
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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)
Bafetinib
BAFETINIB
Benzamide, N-[3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl]-4-[[(3S)-3- (dimethylamino)-1-pyrrolidinyl]methyl]-3-(trifluoromethyl)-
CNS-9
Dual Bcr-Abl/Lyn Tyrosine Kinase Inhibitor INNO-406
INNO-406
NS-187

External Source Codes: 
CAS Registry Number 859212-16-1 (see NLM ChemIDplus info)
FDA UNII Code NVW4Z03I9B
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  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C62516

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