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Description
Background Information:
AZD8186 is a metabolically stable and pharmacologically excellent PI3Kβ/δ isoform-selective inhibitor. It is orally available, potent and selective. Enantiomerically pure AZD8186 inhibits PI3Kβ and PI3Kδ in cellular assays with IC50 values of 3 nM and 17 nM, respectively, highly selective over PI3Kα (IC50 = 752 nM). It has demonstrated a profound pharmacodynamics modulation of p-Akt in PTEN-de?cient PC3 prostate tumor bearing mice after oral administration, and showed a complete inhibition of tumor growth in the mouse PTEN-de?cient PC3 prostate tumor xenograft model (ref. 1).
Reference:
1. B. Barlaam, et al, Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chrom ene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers. J. Med. Chem. 2015, 58, p943−962.
APIM050104: AZD8186
CAS No.: 1627494-13-6.
Molecular Formula: C24H25F2N3O4 ?0.2H2O.
Molecular Weight: 461.1.
Purity: >99.8 Chemical and Enantiomerical Purity (By HPLC and Chiral HPLC).
QC: HPLC, Chiral HPLC, NMR and Quantitative Elemental Analysis.
Solubility: In DMSO.
Storage: Refer to Certificate of Analysis.
Additional information
| Ship from Country | USA |
|---|---|
| Size | 10 mg, 100 mg, 50 mg |