AZD3965 | MCT1 inhibitor

AZD3965 chemical structure

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AZD3965 (1448671-31-5) is a potent inhibitor (Ki’s: 1.6 – 3.2 nM) of monocarboxylate transporter 1 (MCT1) with approximately 6-fold selectivity over MCT2.1 Active in multiple cancer models as monotherapy or in combination with other chemotherapeutics.2 AZD3965 improved CAR-T cell therapy against B-cell malignancies.3 It inhibited lipid biosynthesis and increased tumor infiltration of dendritic and natural killer cells.4 Combination therapy with immune checkpoint blockade suppressed lactate-mediated immunosuppression in the tumor microenvironment.5

References/Citations:

  1. Curtis et al. (2017), Preclinical pharmacology of AZD3965. A selective inhibitor of MCT1: DLBCL, NHL, and Burkitt’s lymphoma antitumor activity; Oncotarget 8 69219
  2. Silva et al. (2021), In Vivo Anticancer Activity of AZD3965: A Systematic Review; Molecules 27 181
  3. Lopez et al. (2023), Inhibition of lactate transport by MCT-1 blockade improves chimeric antigen receptor T-cell therapy against B-cell malignancies; Immunother. Cancer 11 e006287
  4. Beloueche-Babari et al. (2020), Monocarboxylate transporter 1 blockade with AZD3965 inhibits lipid biosynthesis and increases tumour immune cell infiltration; Br. J. Cancer 122 895
  5. Faghihkhorasani et al. (2025), Role of monocarboxylate transporters in cancer immunology and their therapeutic potential; Br. J. Pharmacol. 182 4421
1448671-31-5, AZD-3965, AZD3965, AZD3965 supplier, MCT1 inhibitor

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AZD3965 (1448671-31-5) is a potent inhibitor (Ki’s: 1.6 – 3.2 nM) of monocarboxylate transporter 1 (MCT1) with approximately 6-fold selectivity over MCT2.1 Active in multiple cancer models as monotherapy or in combination with other chemotherapeutics.2 AZD3965 improved CAR-T cell therapy against B-cell malignancies.3 It inhibited lipid biosynthesis and increased tumor infiltration of dendritic and natural killer cells.4 Combination therapy with immune checkpoint blockade suppressed lactate-mediated immunosuppression in the tumor microenvironment.5

References/Citations:

  1. Curtis et al. (2017), Preclinical pharmacology of AZD3965. A selective inhibitor of MCT1: DLBCL, NHL, and Burkitt’s lymphoma antitumor activity; Oncotarget 8 69219
  2. Silva et al. (2021), In Vivo Anticancer Activity of AZD3965: A Systematic Review; Molecules 27 181
  3. Lopez et al. (2023), Inhibition of lactate transport by MCT-1 blockade improves chimeric antigen receptor T-cell therapy against B-cell malignancies; Immunother. Cancer 11 e006287
  4. Beloueche-Babari et al. (2020), Monocarboxylate transporter 1 blockade with AZD3965 inhibits lipid biosynthesis and increases tumour immune cell infiltration; Br. J. Cancer 122 895
  5. Faghihkhorasani et al. (2025), Role of monocarboxylate transporters in cancer immunology and their therapeutic potential; Br. J. Pharmacol. 182 4421