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AZD-8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ. It shows efficacy against PTEN-null tumors, which become dependent on the PI3Kβ isoform. The loss of the PTEN protein results in upregulation of the PI3K/AKT pathway, making small molecules that target PI3Kβ viable in cancers like PTEN-deficient breast and prostate tumors.
| Cas No. | 1627494-13-6 |
|---|---|
| Purity | ≥99% |
| Formula | C24H25F2N3O4 |
| Formula Wt. | 457.48 |
| IUPAC Name | 8-{(1R)-1-[(3,5-Difluorophenyl)amino]ethyl}-N,N-dimethyl-2-(4-morpholinyl)-4-oxo-4H-chromene-6-carboxamide |
| Synonym | AZD 8186, AZD8186 |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Barlaam B., Cosulich S., et al. Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers. J Med Chem. 58(2):943-62 (2015). PMID: 25514658.
Lynch J., Planska U., et al. Inhibiting PI3Kβ with AZD8186 Regulates Key Metabolic Pathways in PTEN-Null Tumors. Clin Cancer Res. 23(24):7584-95 (2017). PMID: 28972046.
Hancox U., Cosulich S., et al. Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel. Mol Cancer Ther. 14(1):48-58 (2015). PMID: 25398829.