AZD8186

Research use only, not for human use.

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 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); inhibits ADP-induced human platelet aggregation with IC50 of 186 nM, shows no significant binding to 442 other kinases; 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); 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; effectively inhibits growth of prostate and TNBC tumors, both as a single agent and in combination with docetaxel.Breast Cancer Phase 1 Clinical

AZD-8186

PI3K/Akt/mTOR signaling

PI3K

PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ

Cancer

Breast Cancer

1627494-13-6

457.47

C24H25F2N3O4

>98% (HPLC)

DMSO: ≥ 35 mg/mL

O=C(N(C)C)C1=CC([C@@H](C)NC2=CC(F)=CC(F)=C2)=C3C(C(C=C(O3)N4CCOCC4)=O)=C1

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

(-20℃)

With Ice Pack

≥ 2 years