AZD3965

  • Chemical Properties
CAS No. 1448671-31-5 Cat. No. BCP17734
Name AZD3965
Synonyms AZD-3965;AZD 3965;
Formula C21H24F3N5O5S M. Wt 515.51
  • Biological Activity
Description AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. In vivo, AZD3965 is well tolerated and induces a dose and time dependent accumulation of lactate in the tumours, suppresses tumour growth and in the Raji model potentiates the effects of Rituxan, doxorubicin and bendamustine. The selective inhibition of lactate transport by the MCT1 inhibitor AZD3965 offers an novel mechanism for targeting the metabolic phenotype in tumours that preferentially express MCT1.
Pathways Ion Channel/Membrane Transporter 
Targets MCT 

Structure

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