AZD 6482

AZD 6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC₅₀s = 0.69, 13.6, 47.8, and 136 nM, respectively).¹ It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.¹ AZD 6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.^1,2,3 AZD 6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.¹ It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.⁴

WARNING This product is not for human or veterinary use.

1. Ni, J., Liu, Q., Xie, S., et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2(5), 425-433 (2012).

2. Weigelt, B., Warne, P.H., Lambros, M.B., et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin. Cancer Res. 19(13), 3533-3544 (2013).

3. Nichols, A.C., Black, M., Yoo, J., et al. Exploiting high-throughput cell line drug screening studies to identify candidate therapeutic agents in head and neck cancer. BMC Pharmacol. Toxicol. 15, (2014).

4. Nylander, S., Kull, B., Björkman, J.A., et al. Human target validation of phosphoinositide 3-kinase (PI3K)β: Effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J. Thromb. Haemost. 10(10), 2127-2136 (2012).