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Chemical Structure : AZD8186
CAS No.: 1627494-13-6
Catalog No.: PC-42978Not For Human Use, Lab Use Only.
AZD8186 is a potent, isoform-specific PI3Kβ inhibitor with IC50 of 4 nM, also inhibits PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | Get quote | ||
| 200 mg | Get quote | ||
| 1 g | Get quote |
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AZD8186 is a potent, isoform-specific PI3Kβ inhibitor with IC50 of 4 nM, also inhibits PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
AZD8186 inhibits ADP-induced human platelet aggregation with IC50 of 186 nM, shows no significant binding to 442 other kinases.
AZD8186 inhibits PI3Kβ-dependent activation of pAKT (Ser473) in MDA-MB-468 cells (IC50=3 nM), inhibits proliferation of MDA-MB-468 cells (GI50=65 nM).
AZD8186 suppresses phosphorylation of AKT, PRAS40, S6, and FOXO with IC50 of <10-300 nM in breast cancer cells, also induces nuclear translocation of FOXO3a in vitro.
AZD8186 effectively inhibits growth of prostate and TNBC tumors, both as a single agent and in combination with docetaxel.
| M.Wt | 457.4698 | |
| Formula | C24H25F2N3O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 35 mg/mL |
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| Chemical Name/SMILES |
4H-1-Benzopyran-6-carboxamide, 8-[(1R)-1-[(3,5-difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo- |
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1. Hancox U, et al. Mol Cancer Ther. 2015 Jan;14(1):48-58.
2. Barlaam B, et al. J Med Chem. 2015 Jan 22;58(2):943-62.
3. Schwartz S, et al. Cancer Cell. 2015 Jan 12;27(1):109-22.
4. Lynch JT, et al. Clin Cancer Res. 2017 Dec 15;23(24):7584-7595.
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