AZD3965

Overview

AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, which is 6-fold selective over MCT2 and does not inhibit MCT4 at 10 μM. Both lactate transport and cell growth are potently inhibited by AZD3965 in lymphoma cell lines that preferentially express MCT1. Lactate transport inhibition in some cell lines also induces a cytotoxic effect. In vitro combination studies show that lactate transport inhibition can enhance the induction of cell death by doxorubicin. Blocking lactate transport in vitro also leads to a rapid inhibition of glucose uptake in the Raji Burkitt's lymphoma cell line. In vivo, AZD3965 is well tolerated and induces a dose- and time-dependent accumulation of lactate in the tumors, suppresses tumor 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 a novel mechanism for targeting the metabolic phenotype in tumors that preferentially express MCT1.

Application

Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cardiovascular and blood system | MCT

Product Information

• Catalog No.: B2693-463251
• CAS No.: 1448671-31-5
• Molecular Formula: C21H24F3N5O5S
• Molecular Weight: 515.51
• Purity: >98%

Source

Original product source