AZD 2014

AZD 2014 is a potent, selective, ATP-competitive mTORC1/2 dual inhibitor that inhibits phosphorylation of both mTORC1 and 2 substrate proteins in whole cells.¹ It exhibits an IC₅₀ value of 2.81 nM against the isolated recombinant enzyme and >1,000-fold selectivity against all PI3K isoforms.¹ AZD 2014 has broad antiproliferative effects across multiple cell lines and reduces tumor growth in in vivo models of ER⁺ breast cancer.¹. It has efficacy against acute myeloid leukemia when combined with the pan Pim kinase inhibitor AZD 1208 (Item No. 20235) and enhances the radiosensitivity of different cancer cell types.^2,3,4

WARNING This product is not for human or veterinary use.

1. Guichard, S.M., Curwen, K., Bihani, T., et al. AZD2014, an inhibitor of mTORC1 and mTORC2, is highly effective in ER+ breast cancer when administered using intermittent or continuous schedules. Mol. Cancer Ther. 14(11), 2508-2518 (2015).

2. Harada, M., Benito, J., Yamamaoto, S., et al. The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Oncotarget 6(35), 37930-37947 (2015).

3. Kahn, J., Hayman, T.J., Jamal, M., et al. The mTORC1/mTORC2 inhibitor AZD2014 enhances the radiosensitivity of glioblastoma stem-like cells. Neuro. Oncol. 16(1), 29-37 (2014).

4. Yu, C.-C., Huang, H.-b., Hung, S.-K., et al. AZD2014 radiosensitizes oral squamous cell carcinoma by inhibiting AKT/mTOR axis and inducing G₁/G₂/M cell cycle arrest. PLoS One 11(3), e0151942 (2016).