RGNCY-0028 (AZD8186)

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AZD8186 is a clinical candidate optimized from a series of  8-(1-anilino)ethyl)-2-morpholino-4-oxo-4H -chromene-6-carboxamides as PI3Kβ /δ  inhibitors.  AZD8186 has high metabolic stability and suitable physical properties for oral administration. It showed profound pharmacodynamic modulation of p-Akt in PTEN deficient PC3 prostate tumor bearing mice after oral administration. It also showed complete inhibition of tumor growth in the mouse PTEN-deficient PC3 prostate tumor xenograft model. AZD8186 was selected as a clinical candidate for treatment of PTEN deficient cancers and has recently entered phase I clinical trials. PI3Kβ IC50 = 0.003μM, PI3Kδ IC50 = 0.017μM, PI3Kα IC50 = 0.752μM.

Systematic Name: (R)-8-(1-((3,5-difluorophenyl)amino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide

SMILES: CN(C)C(C1=CC2=C(OC(N3CCOCC3)=CC2=O)C([C@@H](C)NC4=CC(F)=CC(F)=C4)=C1)=O

Chemical Formula: C24H25F2N3O4

Molecular Weight: 457.48

PMID: 25514658

Reference: Barlaam, Bernard, 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." Journal of Medicinal Chemistry (2014).

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