AZD6482 is an isoform-selective and potent ATP competitive inhibitor of PI3Kb. AZD6482 produces an antithrombotic effect without an increased bleeding time or blood loss in humans and in dogs.
isoform-selective and potent ATP competitive inhibitor of PI3Kb
Clinical cancer research : an official journal of the American Association for Cancer Research, 19(13), 3533-3544 (2013-05-16)
Endometrioid endometrial cancers (EEC) frequently harbor coexisting mutations in phosphoinositide 3-kinase (PI3K) pathway genes, including PTEN, PIK3CA, PIK3R1, and KRAS. We sought to define the genetic determinants of PI3K pathway inhibitor response in EEC cells, and whether PTEN-mutant EEC cell
Journal of thrombosis and haemostasis : JTH, 10(10), 2127-2136 (2012-08-22)
Based on in vitro and animal data, PI3Kβ is given an important role in platelet adhesion and aggregation but its role in insulin signaling is unclear. To strengthen the PI3Kβ target validation using the novel, short-acting inhibitor AZD6482. AZD6482 is
Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine, 37(11), 14831-14839 (2016-09-19)
Breast cancer is one of the leading causes of death for women worldwide. Among various subtypes of breast cancer, human epidermal growth factor receptor 2 (HER2)-positive and phosphatase and tensin homolog (PTEN) loss breast cancer is a cause of great
The PTEN tumor suppressor controls cell death and survival by regulating functions of various molecular targets. While the role of PTEN lipid-phosphatase activity on PtdIns(3,4,5)P3 and inhibition of PI3K pathway is well characterized, the biological relevance of PTEN protein-phosphatase activity
Frequent mutation of PI3K/AKT/mTOR signaling pathway genes in human cancers has stimulated large investments in targeted drugs but clinical successes are rare. As a result, many cancers with high PI3K pathway activity, such as triple-negative breast cancer (TNBC), are treated
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