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AZD8186

Chemical Structure : AZD8186

CAS No.: 1627494-13-6

AZD8186 (AZD-8186)

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).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 457.4698
Formula C24H25F2N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 35 mg/mL

Chemical Name/SMILES

4H-1-Benzopyran-6-carboxamide, 8-[(1R)-1-[(3,5-difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo-

References

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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