| Identification | Back Directory | [Name]
AZD8186 | [CAS]
1627494-13-6 | [Synonyms]
CS-1576
AZD8186
EOS-61540
AZD 8186, >=98%
AZD-8186;AZD 8186
AZD8186;AZD-8186;AZD 8186
8-(1-((3,5-difluorophenyl)amino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide
(R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide
8-[(1R)-1-[(3,5-Difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-6-carboxamide
4H-1-Benzopyran-6-carboxamide, 8-[(1R)-1-[(3,5-difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo- | [Molecular Formula]
C24H25F2N3O4 | [MOL File]
1627494-13-6.mol | [Molecular Weight]
457.47 |
| Chemical Properties | Back Directory | [Melting point ]
226-227°C | [Boiling point ]
645.2±55.0 °C(Predicted) | [density ]
1.351±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
DMSO (Slightly), Ethanol (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
2.56±0.50(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
AZD 8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers. | [Biological Activity]
the pi3k-akt signaling pathway plays a critical role in cell growth, proliferation, motility, and survival. in human cancer, this pathway is activated by several mechanisms, including somatic mutations, deletions, and amplifications. class i pi3ks are further divided into class ia enzymes (pi3kα, pi3kβ, and pi3kδ) and class ib enzymes (pi3kγ). azd8186 is a potent and selective inhibitor of pi3kβ and pi3kδ. | [in vitro]
azd8186 gave potent inhibition of p-akt in cells sensitive to pi3kβ inhibition and in cells sensitive to pi3kδ inhibition but not to cells sensitive to pi3kα inhibition. the overall kinase selectivity of azd8186 was evaluated in several panels of recombinant protein and lipid kinase assays. 13 did not show significant activity against a panel of 59 protein kinases tested at 1 μm [1]. | [in vivo]
the antitumor activity of azd8186 was evaluated in the pten deficient pc3 prostate tumor xenograft model in nude mice, either at 100 mg/kg b.i.d. without abt coadministration, or at 60, 30, and 10 mg/mg b.i.d. with abt coadministration. higher inhibition was seen in the 60 and 30 mg/kg groups with abt coadministration than in the 100 mg/kg group without abt coadministration [1]. | [IC 50]
0.003 μm for pi3kβ and 0.017 μm for pi3kδ | [storage]
Store at -20°C | [References]
[1] barlaam b, cosulich s, degorce s, fitzek m, green s, hancox u, lambert-van der brempt c, lohmann jj, maudet m, morgentin r, pasquet mj, péru a, plé p, saleh t, vautier m, walker m, ward l, warin n. 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. j med chem. 2015 jan 22;58(2):943-62.
[2] https://clinicaltrials. gov/ct2/show/nct01884285?term=azd8186&rank=1 |
|
|